TCS 5861528|TRPA1 channel blocker|DC Chemials
TCS 5861528 is a TRPA1 channel blocker and an antagonizer of AITC- and 4-HNE-evoked calcium influx.
Product name: TCS 5861528 |Cat No. DC8262|Other names: TCS 5861528 ,TCS 5861528,TCS 5861528 |Cas: 332117-28-9|Molecule Weight: 369.42|Molecule Formular: C19H23N5O3| Purity: >98%
Selective TRPA1 channel blocker (IC50 values are 14.3 and 18.7 µM for AITC- and 4-HNE- evoked Ca2+ influx respectively). Exhibits little of no activity at TRPV1 channels. Reduces mechanical hypersensitivity, attenuates diabetes mellitus hypersensitivity and displays antinociceptive properties.
For research and scientific purpose only, not for human use.
2015年6月25日星期四
(-)JQ-1|Negative of +JQ-1|DC CHEMICALS
(-)JQ-1|Negative of +JQ-1|DC CHEMICALS
The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains，it is the negative control of +JQ-1.
Product name: (-)-JQ-1 |Cat No. DC8261|Other names: -JQ-1,-JQ-1 , -JQ-1 |Cas: 1268524-71-5|Molecule Weight: 457|Molecule Formular: C23H25ClN4O2S| Purity: >98%,ee>99%
The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains，it is the negative control of +JQ-1.
For research and scientific purpose only, not for human use.
The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains，it is the negative control of +JQ-1.
Product name: (-)-JQ-1 |Cat No. DC8261|Other names: -JQ-1,-JQ-1 , -JQ-1 |Cas: 1268524-71-5|Molecule Weight: 457|Molecule Formular: C23H25ClN4O2S| Purity: >98%,ee>99%
The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains，it is the negative control of +JQ-1.
For research and scientific purpose only, not for human use.
Exemestane(FCE 24304)|aromatase inhibitor|DC Chemicals
Exemestane(FCE 24304)|aromatase inhibitor|DC Chemicals
Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
Product name: Exemestane(FCE 24304) |Cat No. DC8260|Other names: FCE24304 ,FCE-24304|Cas: 107868-30-4|Molecule Weight: 296.4|Molecule Formular: C20H24O2| Purity: >98%
Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [3H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM. Exemestane (1 μM) increases alkaline phosphatase activity in hFOB and Saos-2 cells and induces the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells. Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells.
Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. Exemestane (100 mg/kg) and 17-hydroexemestane (20 mg/kg) significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin in rats and causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol inOVX rats .Exemestane (20 mg/kg/day s.c.) induces 26% complete (CR) and 18% partial (PR) tumor regressions in rats with 7,12-dimethylbenzanthracene (DMBA)-induced mammary tumors.
For research and scientific purpose only, not for human use.
Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
Product name: Exemestane(FCE 24304) |Cat No. DC8260|Other names: FCE24304 ,FCE-24304|Cas: 107868-30-4|Molecule Weight: 296.4|Molecule Formular: C20H24O2| Purity: >98%
Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [3H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM. Exemestane (1 μM) increases alkaline phosphatase activity in hFOB and Saos-2 cells and induces the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells. Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells.
Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. Exemestane (100 mg/kg) and 17-hydroexemestane (20 mg/kg) significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin in rats and causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol inOVX rats .Exemestane (20 mg/kg/day s.c.) induces 26% complete (CR) and 18% partial (PR) tumor regressions in rats with 7,12-dimethylbenzanthracene (DMBA)-induced mammary tumors.
For research and scientific purpose only, not for human use.
PF0477736|CHK inhibitor|DC Chemicals
PF0477736|CHK inhibitor|DC Chemicals
PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity
Product name: PF0477736 |Cat No. DC8259|Other names: PF 477736 ,PF-477736,PF477736 |Cas: 952021-60-2|Molecule Weight: 419.48|Molecule Formular: C22H25N7O2| Purity: >98%
PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity
For research and scientific purpose only, not for human use.
PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity
Product name: PF0477736 |Cat No. DC8259|Other names: PF 477736 ,PF-477736,PF477736 |Cas: 952021-60-2|Molecule Weight: 419.48|Molecule Formular: C22H25N7O2| Purity: >98%
PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity
For research and scientific purpose only, not for human use.
Baricitinib phosphate|JAK 1 inhibitor|DC Chemicals
Baricitinib phosphate|JAK 1 inhibitor|DC Chemicals
Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.
Product name: Baricitinib phosphate |Cat No. DC8258|Other names: INCB-028050,LY-3009104,INCB 028050,LY 3009104,INCB028050,LY3009104|Cas: 1187595-84-1|Molecule Weight: 469.41|Molecule Formular: C16H20N7O6PS| Purity: >98%
Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.in vitro: INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. Significant efficacy, as assessed by improvements in clinical, histologic and radiographic signs of disease, was achieved in the rat adjuvant arthritis model with doses of INCB028050 providing partial and/or periodic inhibition of JAK1/JAK2 and no inhibition of JAK3.
in vivo: The efficacy following daily oral administration of INCB028050 was assessed at doses of 1, 3, or 10 mg/kg based on its pharmacokinetic profile in this species. Disease severity was assessed periodically, scoring clinical signs of disease. These doses were based on the PK/PD relationship established with the IL-6 WBA, with the goal of inhibiting JAK1/2 signaling by no more than 50% for half of the day. Relative to vehicle-treated animals, increasing doses of INCB028050 inhibited disease scores by 24% (p < 0.05), 57% (p < 0.01), and 81% (p < 0.01), respectively. Baricitinib preferentially inhibits JAK1 and JAK2, with 10-fold selectivity over Tyk2 and 100-fold over JAK3. The observed effects of GLPG-0634 on the ACR20, albeit in a smaller study, appear to be at least as good as that seen with tofacitinib and superior to that of baricitinib, since baricitinib only moderately affect the ACR20 values in Phase IIa clinical studies.
Clinical trial: Baricitinib (LY3009104, INCB28050) against JAK1/JAK2 starting phase IIb for rheumatoid arthritis
For research and scientific purpose only, not for human use.
Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.
Product name: Baricitinib phosphate |Cat No. DC8258|Other names: INCB-028050,LY-3009104,INCB 028050,LY 3009104,INCB028050,LY3009104|Cas: 1187595-84-1|Molecule Weight: 469.41|Molecule Formular: C16H20N7O6PS| Purity: >98%
Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.in vitro: INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. Significant efficacy, as assessed by improvements in clinical, histologic and radiographic signs of disease, was achieved in the rat adjuvant arthritis model with doses of INCB028050 providing partial and/or periodic inhibition of JAK1/JAK2 and no inhibition of JAK3.
in vivo: The efficacy following daily oral administration of INCB028050 was assessed at doses of 1, 3, or 10 mg/kg based on its pharmacokinetic profile in this species. Disease severity was assessed periodically, scoring clinical signs of disease. These doses were based on the PK/PD relationship established with the IL-6 WBA, with the goal of inhibiting JAK1/2 signaling by no more than 50% for half of the day. Relative to vehicle-treated animals, increasing doses of INCB028050 inhibited disease scores by 24% (p < 0.05), 57% (p < 0.01), and 81% (p < 0.01), respectively. Baricitinib preferentially inhibits JAK1 and JAK2, with 10-fold selectivity over Tyk2 and 100-fold over JAK3. The observed effects of GLPG-0634 on the ACR20, albeit in a smaller study, appear to be at least as good as that seen with tofacitinib and superior to that of baricitinib, since baricitinib only moderately affect the ACR20 values in Phase IIa clinical studies.
Clinical trial: Baricitinib (LY3009104, INCB28050) against JAK1/JAK2 starting phase IIb for rheumatoid arthritis
For research and scientific purpose only, not for human use.
GNE 477|PI3K/mTOR inhibitor|DC Chemicals
GNE 477|PI3K/mTOR inhibitor|DC Chemicals
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.
Product name: GNE 477 |Cat No. DC8257|Other names: GNE-477 ,GNE477 |Cas: 1032754-81-6|Molecule Weight: 504.63|Molecule Formular: C21H28N8O3S2| Purity: >98%
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.GNE-477 is a potent dual PI3K/mTOR inhibitor that displays desirable pharmacokinetic properties in each of three species studied. GNE-477 also exhibited stasis in a PC3 tumor growth inhibition study.
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.
Product name: GNE 477 |Cat No. DC8257|Other names: GNE-477 ,GNE477 |Cas: 1032754-81-6|Molecule Weight: 504.63|Molecule Formular: C21H28N8O3S2| Purity: >98%
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.GNE-477 is a potent dual PI3K/mTOR inhibitor that displays desirable pharmacokinetic properties in each of three species studied. GNE-477 also exhibited stasis in a PC3 tumor growth inhibition study.
For research and scientific purpose only, not for human use.
AS 602801(Bentamapimod)|JNK Inhibitor|DC Chemicals
AS 602801(Bentamapimod)|JNK Inhibitor|DC Chemicals
AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.
Product name: AS 602801(Bentamapimod) |Cat No. DC8256|Other names: AS-602801 ,Bentamapimod ,AS602801|Cas: 848344-36-5|Molecule Weight: 457.55|Molecule Formular: C25H23N5O2S| Purity: >98%
AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.In activated PBMCs from HVs, we showed that AS602801 blocked T-lymphocyte proliferation and induced apoptosis. In RRMS CD4+ and CD8+ cells, AS602801 induced apoptosis genes and expression of surface markers, while in RRMS CD11b+ cells it induced expression of innate immunity receptors and co-stimulatory molecules. Untreated cells from RRMS active-phase patients significantly released interleukin-23 (IL-23) and interferon-gamma (IFN-γ) and expressed less apoptosis markers compared to the cells of HVs.
For research and scientific purpose only, not for human use.
AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.
Product name: AS 602801(Bentamapimod) |Cat No. DC8256|Other names: AS-602801 ,Bentamapimod ,AS602801|Cas: 848344-36-5|Molecule Weight: 457.55|Molecule Formular: C25H23N5O2S| Purity: >98%
AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.In activated PBMCs from HVs, we showed that AS602801 blocked T-lymphocyte proliferation and induced apoptosis. In RRMS CD4+ and CD8+ cells, AS602801 induced apoptosis genes and expression of surface markers, while in RRMS CD11b+ cells it induced expression of innate immunity receptors and co-stimulatory molecules. Untreated cells from RRMS active-phase patients significantly released interleukin-23 (IL-23) and interferon-gamma (IFN-γ) and expressed less apoptosis markers compared to the cells of HVs.
For research and scientific purpose only, not for human use.
SD-06| p38 MAPK inhibitor|DC Chemicals
SD-06| p38 MAPK inhibitor|DC Chemicals
SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po).
Product name: SD-06 |Cat No. DC8255|Other names: SD-06 ,SD 06 ,SD06 |Cas: 271576-80-8|Molecule Weight: 397.86|Molecule Formular: C20H20ClN5O2| Purity: >98%
SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po).
For research and scientific purpose only, not for human use.
SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po).
Product name: SD-06 |Cat No. DC8255|Other names: SD-06 ,SD 06 ,SD06 |Cas: 271576-80-8|Molecule Weight: 397.86|Molecule Formular: C20H20ClN5O2| Purity: >98%
SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po).
For research and scientific purpose only, not for human use.
PIK-93|PI4K (PI4KIIIβ) inhibitor|DC Chemicals
PIK-93|PI4K (PI4KIIIβ) inhibitor|DC Chemicals
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM.
Product name: PIK-93 |Cat No. DC8254|Other names: PIK-93,PIK 93,PIK93 |Cas: 593960-11-3|Molecule Weight: 389.88|Molecule Formular: C14H16ClN3O4S2| Purity: >98%
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM.PIK-93 is a PI4KIIIβ inhibitor (IC50 at 19 nM). PIK-93 is the first reported PI4-kinase inhibitor, which is able to inhibit PI4KIIIβ at low-nanomolar range. In addition, PIK-93 also inhibits potently PI3Kγ in vitro (IC50 at 16 nM). PIK-93 inhibits p110α, p110β, p110δwith IC50 of 0.039, 0.59, 0.12 μM. PIK-93 also displays the typical hydrogen bonding to the backbone amide of Val882, and additional ones to the backbone carbonyl of Val882 and between its sulphonamide and Asp964.
For research and scientific purpose only, not for human use.
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM.
Product name: PIK-93 |Cat No. DC8254|Other names: PIK-93,PIK 93,PIK93 |Cas: 593960-11-3|Molecule Weight: 389.88|Molecule Formular: C14H16ClN3O4S2| Purity: >98%
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM.PIK-93 is a PI4KIIIβ inhibitor (IC50 at 19 nM). PIK-93 is the first reported PI4-kinase inhibitor, which is able to inhibit PI4KIIIβ at low-nanomolar range. In addition, PIK-93 also inhibits potently PI3Kγ in vitro (IC50 at 16 nM). PIK-93 inhibits p110α, p110β, p110δwith IC50 of 0.039, 0.59, 0.12 μM. PIK-93 also displays the typical hydrogen bonding to the backbone amide of Val882, and additional ones to the backbone carbonyl of Val882 and between its sulphonamide and Asp964.
For research and scientific purpose only, not for human use.
AV-412(MP-412)|EGFR/ErbB2 dual inhibitor|DC Chemicals
AV-412(MP-412)|EGFR/ErbB2 dual inhibitor|DC Chemicals
AV-412(MP-412) is a potent dual inhibitor of EGFR and ErbB2(IC50=19 nM) tyrosine kinases, including the mutant EGFR(L858R IC50=0.51 nM, T790M IC50=0.79 nM); inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively.
Product name: AV-412(MP-412) |Cat No. DC8253|Other names: AV-412 ,MP-412 ,AV 412 ,MP 412,AV412,MP412|Cas: 451492-95-8|Molecule Weight: 507|Molecule Formular: C27H28ClFN6O| Purity: >98%
AV-412(MP-412) is a potent dual inhibitor of EGFR and ErbB2(IC50=19 nM) tyrosine kinases, including the mutant EGFR(L858R IC50=0.51 nM, T790M IC50=0.79 nM); inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. in vitro: MP-412 (AV-412) is a potent dual inhibitor of EGFR and ErbB2 tyrosine kinases, including the mutant EGFR(L858R,T790M), which is clinically resistant to the EGFR-specific kinase inhibitors erlotinib and gefitinib. In an enzyme assay, MP-412 inhibited the EGFR variants and ErbB2 in the nanomolar range with over 100-fold selectivity compared with other kinases, apart from abl and flt-1, which were both moderately sensitive to the compound. In cells, MP-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100 nM. Moreover, MP-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. MP-412 inhibited phosphorylation of EGFR and its downstream signaling in NCI-H1650 and NCI-H1975 cell lines, which harbor the E746-A750 deletion and L858R + T790M point mutations, respectively, in EGFR . In MCF7 cells, MP-412 depleted not only ErbB2 but also estrogen receptor (ER)-α, and to some extent, affected Raf-1, while MP-412 activated Hsp70 expression. MP-412 increased immunocomplexing of Hsp70 with ErbB2 and ER-α, with simultaneous induction of ubiquitination of these client proteins. Furthermore, in combination with proteasome inhibitor, MP-412 resulted in the noticeable accumulation of ErbB2 and ER-α in the detergent insoluble fraction of cell lysates.
in vivo: In animal studies using cancer xenograft models, MP-412 (30 mg/kg) demonstrated complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. MP-412 suppressed autophosphorylation of EGFR and ErbB2 at the dose corresponding to its antitumor efficacy. MP-412 showed a significant antitumor effect on the ErbB2-overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib. MP-412 showed potent activity in KPL-4 and DU145 xenografts, in which lapatinib was ineffective. MP-412 also inhibited tumor models in which conventional chemotherapies were less effective.
For research and scientific purpose only, not for human use.
AV-412(MP-412) is a potent dual inhibitor of EGFR and ErbB2(IC50=19 nM) tyrosine kinases, including the mutant EGFR(L858R IC50=0.51 nM, T790M IC50=0.79 nM); inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively.
Product name: AV-412(MP-412) |Cat No. DC8253|Other names: AV-412 ,MP-412 ,AV 412 ,MP 412,AV412,MP412|Cas: 451492-95-8|Molecule Weight: 507|Molecule Formular: C27H28ClFN6O| Purity: >98%
AV-412(MP-412) is a potent dual inhibitor of EGFR and ErbB2(IC50=19 nM) tyrosine kinases, including the mutant EGFR(L858R IC50=0.51 nM, T790M IC50=0.79 nM); inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. in vitro: MP-412 (AV-412) is a potent dual inhibitor of EGFR and ErbB2 tyrosine kinases, including the mutant EGFR(L858R,T790M), which is clinically resistant to the EGFR-specific kinase inhibitors erlotinib and gefitinib. In an enzyme assay, MP-412 inhibited the EGFR variants and ErbB2 in the nanomolar range with over 100-fold selectivity compared with other kinases, apart from abl and flt-1, which were both moderately sensitive to the compound. In cells, MP-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100 nM. Moreover, MP-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. MP-412 inhibited phosphorylation of EGFR and its downstream signaling in NCI-H1650 and NCI-H1975 cell lines, which harbor the E746-A750 deletion and L858R + T790M point mutations, respectively, in EGFR . In MCF7 cells, MP-412 depleted not only ErbB2 but also estrogen receptor (ER)-α, and to some extent, affected Raf-1, while MP-412 activated Hsp70 expression. MP-412 increased immunocomplexing of Hsp70 with ErbB2 and ER-α, with simultaneous induction of ubiquitination of these client proteins. Furthermore, in combination with proteasome inhibitor, MP-412 resulted in the noticeable accumulation of ErbB2 and ER-α in the detergent insoluble fraction of cell lysates.
in vivo: In animal studies using cancer xenograft models, MP-412 (30 mg/kg) demonstrated complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. MP-412 suppressed autophosphorylation of EGFR and ErbB2 at the dose corresponding to its antitumor efficacy. MP-412 showed a significant antitumor effect on the ErbB2-overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib. MP-412 showed potent activity in KPL-4 and DU145 xenografts, in which lapatinib was ineffective. MP-412 also inhibited tumor models in which conventional chemotherapies were less effective.
For research and scientific purpose only, not for human use.
Vorinostat (SAHA)|HDAC Inhibitor|DC Chemicals
Vorinostat (SAHA)|HDAC Inhibitor|DC Chemicals
Vorinostat (SAHA) is an HDAC1/3 inhibitor with IC50 of ~10 nM.
Product name: Vorinostat (SAHA) |Cat No. DC8252|Other names: Vorinostat,SAHA |Cas: 149647-78-9|Molecule Weight: 264.32|Molecule Formular: C14H20N2O3| Purity: >98%
Vorinostat (SAHA) is an HDAC1/3 inhibitor with IC50 of ~10 nM.in vitro: Vorinostat inhibits the activities of HDAC1 and HDAC3 with IC50 of 10 nM and 20 nM, respectively. Vorinostat also results in a marked hyperacetylation of histone H4. Vorinostat inhibits the growth of three prostate cancer cell lines LNCaP, PC-3 and TSU-Pr1 at micromolar concentrations (2.5-7.5 μM), and induces dose-dependent cell death in LNCaP cells. Vorinostat treatment in MCF-7 cells inhibits cell proliferation at an IC50 of 0.75 μM resulting in the accumulation of cells in the G1 and G2-M phase of the cell cycle. Vorinostat also induces differentiation in the estrogen receptor-negative cell line SKBr-3 and the retinoblastoma-negative cell line MDA-468. Vorinostat treatment at 1 μM for 8 hours or more is sufficient to irreversibly induce apoptosis of human multiple myeloma (MM) cells. The gene expression profiles of Vorinostat treated MM cells are not hallmarked by global transcriptional activation, but by coordinated transcriptional changes of specific functional groups of genes such as cytokine-induced proliferative/survival signaling cascades, oncogenes-tumor suppressor genes, regulators of apoptosis, DNA synthesis-repair and cell cycle, and proteasome-ubiquitin function.
in vivo: Administration of Vorinostat (~100 mg/kg/day) significantly inhibits the growth of CWR22 human prostate xenografts in nude mice with tumor reductions of 78%, 97% and 97%, at doses of 25 mg/kg/day, 50 mg/kg/day and 100 mg/kg/day, respectively, compared with control. Vorinostat induces the accumulation of acetylated core histones and prostate-specific antigen mRNA expression in CWR22 cells, resulting in higher levels of serum prostate-specific antigen than predicted from tumor volume alone. Oral administration of Vorinostat (0.67g/L) crosses the blood-brain barrier, increases histone acetylation in the brain, and dramatically improves the motor impairment in the R6/2 mice model of Huntington's disease.
Vorinostat (SAHA) is an HDAC1/3 inhibitor with IC50 of ~10 nM.
Product name: Vorinostat (SAHA) |Cat No. DC8252|Other names: Vorinostat,SAHA |Cas: 149647-78-9|Molecule Weight: 264.32|Molecule Formular: C14H20N2O3| Purity: >98%
Vorinostat (SAHA) is an HDAC1/3 inhibitor with IC50 of ~10 nM.in vitro: Vorinostat inhibits the activities of HDAC1 and HDAC3 with IC50 of 10 nM and 20 nM, respectively. Vorinostat also results in a marked hyperacetylation of histone H4. Vorinostat inhibits the growth of three prostate cancer cell lines LNCaP, PC-3 and TSU-Pr1 at micromolar concentrations (2.5-7.5 μM), and induces dose-dependent cell death in LNCaP cells. Vorinostat treatment in MCF-7 cells inhibits cell proliferation at an IC50 of 0.75 μM resulting in the accumulation of cells in the G1 and G2-M phase of the cell cycle. Vorinostat also induces differentiation in the estrogen receptor-negative cell line SKBr-3 and the retinoblastoma-negative cell line MDA-468. Vorinostat treatment at 1 μM for 8 hours or more is sufficient to irreversibly induce apoptosis of human multiple myeloma (MM) cells. The gene expression profiles of Vorinostat treated MM cells are not hallmarked by global transcriptional activation, but by coordinated transcriptional changes of specific functional groups of genes such as cytokine-induced proliferative/survival signaling cascades, oncogenes-tumor suppressor genes, regulators of apoptosis, DNA synthesis-repair and cell cycle, and proteasome-ubiquitin function.
in vivo: Administration of Vorinostat (~100 mg/kg/day) significantly inhibits the growth of CWR22 human prostate xenografts in nude mice with tumor reductions of 78%, 97% and 97%, at doses of 25 mg/kg/day, 50 mg/kg/day and 100 mg/kg/day, respectively, compared with control. Vorinostat induces the accumulation of acetylated core histones and prostate-specific antigen mRNA expression in CWR22 cells, resulting in higher levels of serum prostate-specific antigen than predicted from tumor volume alone. Oral administration of Vorinostat (0.67g/L) crosses the blood-brain barrier, increases histone acetylation in the brain, and dramatically improves the motor impairment in the R6/2 mice model of Huntington's disease.
For research and scientific purpose only, not for human use.
CP-724,714| HER2/ErbB2 Inhibitor|DC Chemicals
CP-724,714| HER2/ErbB2 Inhibitor|DC Chemicals
CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc. Phase 2.
Product name: CP-724,714 |Cat No. DC8251|Other names: CP-724,714,CP724,714 ,CP 724714,CP 724,714,CP724714,CP-724714|Cas: 383432-38-0|Molecule Weight: 469.54|Molecule Formular: C27H27N5O3| Purity: >98%
CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc. Phase 2.in vitro: CP-724,714 is marked selectively against EGFR with IC50 of 6.4 μM. CP-724,714 is >1,000-fold less potent for IR, IGF-1R, PDGFRβ, VGFR2, abl. Src, c-Met c-jun NH2-terminal kinase (JNK)-2, JNK-3, ZAP-70, cyclin-dependent kinase (CDK)-2, and CDK-5. CP-724,714 potently reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain with IC50 of 32 nM, but is markedly less potent against EGFR in transfected NIH3T3 cells. CP-724,714 sensitively inhibits the proliferation of erbB2-amplified cells including BT-474 and SKBR3, with IC50 of 0.25 and 0.95 μM. CP-724,714 induces the accumulation of cells in G1 phase and a marked reduction in S-phase in BT-474 cells at 1 μM. CP-724,714 likely exerts its hepatotoxicity via both hepatocellular injury and hepatobiliary cholestatic mechanisms. CP-724,714 displays inhibition of cholyl-lysyl fluorescein and taurocholate (TC) efflux into canaliculi in cryopreserved and fresh cultured human hepatocytes, respectively. CP-724,714 inhibits TC transport in membrane vesicles expressing human bile salt export pump with IC50 of 16 μM and inhibits the major efflux transporter in bile canaliculi, MDR1, with IC50 of ~28 μM.
in vivo: CP-724,714 (25 mg/kg) is rapidly absorbed after p.o. administration and causes reduction of tumor erbB2 receptor phosphorylation after dosing in FRE-erbB2 or BT-474 xenografts. CP-724,714 induces apoptosis in FRE-erbB2 xenograft–bearing (s.c.) mice and shows 50% tumor growth inhibition at 50 mg/kg, without weight loss or mortality. CP-724,714 also has great antitumor activity in MDA-MB-453, MDA-MB-231, LoVo (colon), and Colo-205 (colon) xenografts. Furthermore, CP-724,714 (30 or 100 mg/kg) reduces the extracellular signal–regulated kinase and Akt phosphorylation in BT-474 xenografts.
For research and scientific purpose only, not for human use.
CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc. Phase 2.
Product name: CP-724,714 |Cat No. DC8251|Other names: CP-724,714,CP724,714 ,CP 724714,CP 724,714,CP724714,CP-724714|Cas: 383432-38-0|Molecule Weight: 469.54|Molecule Formular: C27H27N5O3| Purity: >98%
CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc. Phase 2.in vitro: CP-724,714 is marked selectively against EGFR with IC50 of 6.4 μM. CP-724,714 is >1,000-fold less potent for IR, IGF-1R, PDGFRβ, VGFR2, abl. Src, c-Met c-jun NH2-terminal kinase (JNK)-2, JNK-3, ZAP-70, cyclin-dependent kinase (CDK)-2, and CDK-5. CP-724,714 potently reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain with IC50 of 32 nM, but is markedly less potent against EGFR in transfected NIH3T3 cells. CP-724,714 sensitively inhibits the proliferation of erbB2-amplified cells including BT-474 and SKBR3, with IC50 of 0.25 and 0.95 μM. CP-724,714 induces the accumulation of cells in G1 phase and a marked reduction in S-phase in BT-474 cells at 1 μM. CP-724,714 likely exerts its hepatotoxicity via both hepatocellular injury and hepatobiliary cholestatic mechanisms. CP-724,714 displays inhibition of cholyl-lysyl fluorescein and taurocholate (TC) efflux into canaliculi in cryopreserved and fresh cultured human hepatocytes, respectively. CP-724,714 inhibits TC transport in membrane vesicles expressing human bile salt export pump with IC50 of 16 μM and inhibits the major efflux transporter in bile canaliculi, MDR1, with IC50 of ~28 μM.
in vivo: CP-724,714 (25 mg/kg) is rapidly absorbed after p.o. administration and causes reduction of tumor erbB2 receptor phosphorylation after dosing in FRE-erbB2 or BT-474 xenografts. CP-724,714 induces apoptosis in FRE-erbB2 xenograft–bearing (s.c.) mice and shows 50% tumor growth inhibition at 50 mg/kg, without weight loss or mortality. CP-724,714 also has great antitumor activity in MDA-MB-453, MDA-MB-231, LoVo (colon), and Colo-205 (colon) xenografts. Furthermore, CP-724,714 (30 or 100 mg/kg) reduces the extracellular signal–regulated kinase and Akt phosphorylation in BT-474 xenografts.
For research and scientific purpose only, not for human use.
MF498|EP4 inhibitor|DC Chemicals
MF498|EP4 inhibitor|DC Chemicals
MF498 is a novel and selective E prostanoid receptor 4 (EP4) inhibitor, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis.
Product name: MF498 |Cat No. DC8249|Other names: MF498,MF-498,MF 498|Cas: 915191-42-3|Molecule Weight: 603.7|Molecule Formular: C32H33N3O7S| Purity: >98%
MF498 is a selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors).In HEK293 cells expressing the human EP4 receptor, MF498 inhibits EP ligand induced activity with an IC50 value of 1.7 nM.In various animal models for arthritis, MF498 has been shown to inhibit inflammation without gastrointestinal toxicity (ED50 values as low as 0.02 mg/kg/day).
For research and scientific purpose only, not for human use.
MF498 is a novel and selective E prostanoid receptor 4 (EP4) inhibitor, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis.
Product name: MF498 |Cat No. DC8249|Other names: MF498,MF-498,MF 498|Cas: 915191-42-3|Molecule Weight: 603.7|Molecule Formular: C32H33N3O7S| Purity: >98%
MF498 is a selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors).In HEK293 cells expressing the human EP4 receptor, MF498 inhibits EP ligand induced activity with an IC50 value of 1.7 nM.In various animal models for arthritis, MF498 has been shown to inhibit inflammation without gastrointestinal toxicity (ED50 values as low as 0.02 mg/kg/day).
For research and scientific purpose only, not for human use.
Ostarine(MK-2286)|androgen receptor modulator (SARM)|DC Chemicals
Ostarine(MK-2286)|androgen receptor modulator (SARM)|DC Chemicals
Ostarine(MK-2866; GTX-024)A modulator to human androgen receptor.
Product name: Ostarine(MK-2286) |Cat No. DC8248|Other names: Ostarine,MK-2866,GTX-024|Cas: 841205-47-8|Molecule Weight: 389.33|Molecule Formular: C19H14F3N3O3| Purity: >98%
Ostarine (MK-2866) is an androgen receptor modulator (SARM) with an ED50 of 0.44 mg/day. Ostarine (MK-2866) has anabolic activity. Lack of PSA increases in men and hair growth in women further corroborated selective anabolic effects of Ostarine (MK-2866). Ostarine (MK-2866) also resulted in a dose-dependent decrease in LDL and HDL cholesterol levels, with the average LDL/HDL ratio for all doses remaining in the low cardiovascular risk catergory.
For research and scientific purpose only, not for human use.
Ostarine(MK-2866; GTX-024)A modulator to human androgen receptor.
Product name: Ostarine(MK-2286) |Cat No. DC8248|Other names: Ostarine,MK-2866,GTX-024|Cas: 841205-47-8|Molecule Weight: 389.33|Molecule Formular: C19H14F3N3O3| Purity: >98%
Ostarine (MK-2866) is an androgen receptor modulator (SARM) with an ED50 of 0.44 mg/day. Ostarine (MK-2866) has anabolic activity. Lack of PSA increases in men and hair growth in women further corroborated selective anabolic effects of Ostarine (MK-2866). Ostarine (MK-2866) also resulted in a dose-dependent decrease in LDL and HDL cholesterol levels, with the average LDL/HDL ratio for all doses remaining in the low cardiovascular risk catergory.
For research and scientific purpose only, not for human use.
KNK437|Pan hsp inhibitor|DC Chemicals
KNK437|Pan hsp inhibitor|DC Chemicals
KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
Product name: KNK437 |Cat No. DC8247|Other names: KNK437,KNK 437|Cas: 218924-25-5|Molecule Weight: 245.23|Molecule Formular: C13H11NO4| Purity: >98%
KNK437 dose-dependently inhibits the acquisition of thermotolerance and the induction of various HSPs including HSP105, HSP70, and HSP40 in COLO 320DM (human colon carcinoma) cells.[1] KNK437 and quercetin inhibits thermotolerance in a dose-dependent manner in PC-3 cells. KNK437 decreases heat-induced accumulation of Hsp70 mRNA and protein in PC-3 and LNCaP cells.KNK437 (200 mg/kg, i.p.) shows no antitumor effects and does not increase the thermosensitivity of nontolerant tumors. The same dose of KNK437 enhances the antitumor effects of fractionated heat treatment in a synergistic manner.[
For research and scientific purpose only, not for human use.
KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
Product name: KNK437 |Cat No. DC8247|Other names: KNK437,KNK 437|Cas: 218924-25-5|Molecule Weight: 245.23|Molecule Formular: C13H11NO4| Purity: >98%
KNK437 dose-dependently inhibits the acquisition of thermotolerance and the induction of various HSPs including HSP105, HSP70, and HSP40 in COLO 320DM (human colon carcinoma) cells.[1] KNK437 and quercetin inhibits thermotolerance in a dose-dependent manner in PC-3 cells. KNK437 decreases heat-induced accumulation of Hsp70 mRNA and protein in PC-3 and LNCaP cells.KNK437 (200 mg/kg, i.p.) shows no antitumor effects and does not increase the thermosensitivity of nontolerant tumors. The same dose of KNK437 enhances the antitumor effects of fractionated heat treatment in a synergistic manner.[
For research and scientific purpose only, not for human use.
MI-3 (ML3,Menin-MLL Inhibitor)|DC Chemicals
MI-3 (ML3,Menin-MLL Inhibitor)|DC Chemicals
MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
Product name: MI-3 (Menin-MLL Inhibitor) |Cat No. DC8246|Other names: MI-3，MI3|Cas: 1271738-59-0|Molecule Weight: 375.55|Molecule Formular: C18H25N5S2| Purity: >98%
In HEK293 cells, MI-3 accesses the protein target and effectively inhibits the menin-MLL-AF9 interaction. MI-3 effectively blocks MLL fusion protein-mediated leukemic transformation by downregulating the expression of target genes required for MLL fusion protein oncogenic activity. In human MLL leukemia cell lines harboring different MLL translocations, MI-3 effectively blocks cell proliferation, and induces apoptosis.
For research and scientific purpose only, not for human use.
MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
Product name: MI-3 (Menin-MLL Inhibitor) |Cat No. DC8246|Other names: MI-3，MI3|Cas: 1271738-59-0|Molecule Weight: 375.55|Molecule Formular: C18H25N5S2| Purity: >98%
In HEK293 cells, MI-3 accesses the protein target and effectively inhibits the menin-MLL-AF9 interaction. MI-3 effectively blocks MLL fusion protein-mediated leukemic transformation by downregulating the expression of target genes required for MLL fusion protein oncogenic activity. In human MLL leukemia cell lines harboring different MLL translocations, MI-3 effectively blocks cell proliferation, and induces apoptosis.
For research and scientific purpose only, not for human use.
4E1RCat|DC Chemicals
4E1RCat|DC Chemicals
4E1RCat is an inhibitor of protein translation that has been shown to prevent eIF4E:eIF4G and eIF4E:4E-BP1 interaction.
Product name: 4E1rcat |Cat No. DC8245|Other names: 4E1RCat|Cas: 328998-25-0|Molecule Weight: 478.45|Molecule Formular: C28H18N2O6| Purity: >98%
Inhibitor of protein translation; blocks eIF4E:eIF4G and eIF4E:4E-BP1 interaction. Prevents assembly of the eIF4F complex and inhibits cap-dependent translation (IC50 ~4 μM). Exhibits chemosensitizing properties.
For research and scientific purpose only, not for human use.
4E1RCat is an inhibitor of protein translation that has been shown to prevent eIF4E:eIF4G and eIF4E:4E-BP1 interaction.
Product name: 4E1rcat |Cat No. DC8245|Other names: 4E1RCat|Cas: 328998-25-0|Molecule Weight: 478.45|Molecule Formular: C28H18N2O6| Purity: >98%
Inhibitor of protein translation; blocks eIF4E:eIF4G and eIF4E:4E-BP1 interaction. Prevents assembly of the eIF4F complex and inhibits cap-dependent translation (IC50 ~4 μM). Exhibits chemosensitizing properties.
For research and scientific purpose only, not for human use.
wp1066（STAT Inhibitor III）|DC Chemicals
wp1066（STAT Inhibitor III）|DC Chemicals
WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT.
Product name: wp1066（STAT Inhibitor III） |Cat No. DC8244|Other names: wp1066, wp 1066,wp-1066|Cas: 857064-38-1|Molecule Weight: 356.2|Molecule Formular: C17H14BrN3O| Purity: >98%
WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells when given at a concentration of 10 µM.1 It also induces apoptosis in U87-MG (IC50 = 5.6 µM) and U373-MG (IC50 = 3.7 µM) cells.WP1066 is orally bioavailable, crosses the blood-brain barrier, and demonstrates in vivo activity, including immune activation as indicated by the up-regulation of CD80 and CD86 and the induction of proliferation of effector T cells. In addition to inducing apoptosis in cancer cells, WP1066 suppresses vascular smooth muscle cell proliferation after vascular injury in mice and prevents seizures following brain injury in rats.
For research and scientific purpose only, not for human use.
WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT.
Product name: wp1066（STAT Inhibitor III） |Cat No. DC8244|Other names: wp1066, wp 1066,wp-1066|Cas: 857064-38-1|Molecule Weight: 356.2|Molecule Formular: C17H14BrN3O| Purity: >98%
WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells when given at a concentration of 10 µM.1 It also induces apoptosis in U87-MG (IC50 = 5.6 µM) and U373-MG (IC50 = 3.7 µM) cells.WP1066 is orally bioavailable, crosses the blood-brain barrier, and demonstrates in vivo activity, including immune activation as indicated by the up-regulation of CD80 and CD86 and the induction of proliferation of effector T cells. In addition to inducing apoptosis in cancer cells, WP1066 suppresses vascular smooth muscle cell proliferation after vascular injury in mice and prevents seizures following brain injury in rats.
For research and scientific purpose only, not for human use.
Pimecrolimus|From DC Chemicals
Pimecrolimus|From DC Chemicals
Pimecrolimus is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12.
Product name: Pimecrolimus |Cat No. DC8243|Other names: Pimecrolimus ， Pimecrolimus，Pimecrolimus |Cas: 137071-32-0 |Molecule Weight: 810.459|Molecule Formular: C43H68ClNO11| Purity: >98%
Pimecrolimus is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12.
Pimecrolimus blocks T-lymphocyte activation pathway by inhibiting calcineurin function. Pimecrolimus prevents the release of cytokines and pro-inflammatory mediators from mast cells. Pimecrolimus binds to macrophilin-12, the pimecrolimusmacrophilin complex then binds to the cytosolic enzyme calcineurin phosphatase. The pimecrolimus-macrophilin complex prevents the dephosphorylation of the cytoplasmic component of the nuclear factor of activated T cells by inhibiting the action of calcineurin. Pimecrolimus inhibits not only the transcription and synthesis of cytokines from mast cells, but also the release of preformed mediators serotonin and β-hexosaminidase by the inhibition of Fc∈-RI-mediated degranulation and secretion. Pimecrolimus treatment causes a strong down-regulation of the expression of mRNA for genes associated with the macrolactam target pathway and inflammation.
Pimecrolimus is found to be as effective as cyclosporine A following oral ingestion and slightly superior after subcutaneous administration in mice. Pimecrolimus contrasts cyclosporine A and tacrolimus by inhibiting ongoing secondary inflammatory response, but not impairing the primary immune response in allergic contact dermatitis in mice. [2] Pimecrolimus is as effective as the high-potency corticosteroid clobetasol-17-propionate in a pig model of allergic contact dermatitis (ACD). Pimecrolimus also effectively reduces skin inflammation and pruritus in hypomagnesemic hairless rats, a model that mimics acute signs of atopic dermatitis [3].
For research and scientific purpose only, not for human use.
Pimecrolimus is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12.
Product name: Pimecrolimus |Cat No. DC8243|Other names: Pimecrolimus ， Pimecrolimus，Pimecrolimus |Cas: 137071-32-0 |Molecule Weight: 810.459|Molecule Formular: C43H68ClNO11| Purity: >98%
Pimecrolimus is an immunophilin ligand, which binds specifically to the cytosolic receptor, immunophilin macrophilin-12.
Pimecrolimus blocks T-lymphocyte activation pathway by inhibiting calcineurin function. Pimecrolimus prevents the release of cytokines and pro-inflammatory mediators from mast cells. Pimecrolimus binds to macrophilin-12, the pimecrolimusmacrophilin complex then binds to the cytosolic enzyme calcineurin phosphatase. The pimecrolimus-macrophilin complex prevents the dephosphorylation of the cytoplasmic component of the nuclear factor of activated T cells by inhibiting the action of calcineurin. Pimecrolimus inhibits not only the transcription and synthesis of cytokines from mast cells, but also the release of preformed mediators serotonin and β-hexosaminidase by the inhibition of Fc∈-RI-mediated degranulation and secretion. Pimecrolimus treatment causes a strong down-regulation of the expression of mRNA for genes associated with the macrolactam target pathway and inflammation.
Pimecrolimus is found to be as effective as cyclosporine A following oral ingestion and slightly superior after subcutaneous administration in mice. Pimecrolimus contrasts cyclosporine A and tacrolimus by inhibiting ongoing secondary inflammatory response, but not impairing the primary immune response in allergic contact dermatitis in mice. [2] Pimecrolimus is as effective as the high-potency corticosteroid clobetasol-17-propionate in a pig model of allergic contact dermatitis (ACD). Pimecrolimus also effectively reduces skin inflammation and pruritus in hypomagnesemic hairless rats, a model that mimics acute signs of atopic dermatitis [3].
For research and scientific purpose only, not for human use.
Eletriptan|From DC Chemicals
Eletriptan|From DC Chemicals
Eletriptan hydrobromide is a orally active, selective 5-HT1B/1D receptor agonist.Eletriptan hydrobromide produces a dose-dependent reduction in carotid artery blood flow in vivo. Displays antimigraine activity.
Product name: Eletriptan hydrobromide |Cat No. DC8242|Other names: Eletriptan,Eletriptan ,Eletriptan |Cas: 177834-92-3|Molecule Weight: 463.43|Molecule Formular: C22H27BrN2O2S| Purity: >98%
Eletriptan hydrobromide is a orally active, selective 5-HT1B/1D receptor agonist.Eletriptan hydrobromide produces a dose-dependent reduction in carotid artery blood flow in vivo. Displays antimigraine activity.
For research and scientific purpose only, not for human use.
Eletriptan hydrobromide is a orally active, selective 5-HT1B/1D receptor agonist.Eletriptan hydrobromide produces a dose-dependent reduction in carotid artery blood flow in vivo. Displays antimigraine activity.
Product name: Eletriptan hydrobromide |Cat No. DC8242|Other names: Eletriptan,Eletriptan ,Eletriptan |Cas: 177834-92-3|Molecule Weight: 463.43|Molecule Formular: C22H27BrN2O2S| Purity: >98%
Eletriptan hydrobromide is a orally active, selective 5-HT1B/1D receptor agonist.Eletriptan hydrobromide produces a dose-dependent reduction in carotid artery blood flow in vivo. Displays antimigraine activity.
For research and scientific purpose only, not for human use.
Ansamitocin P-3|DC Chemicals
Ansamitocin P-3|DC Chemicals
Ansamitocin P-3, a potent anti-tumor maytansinoid found in Actinosynnema pretiosum, is a maytansine analog which displays potent cytotoxicity against the human solid tumor cell lines A-549 and HT-29.
Product name: Ansamitocin P-3 |Cat No. DC8241|Other names: Ansamitocin P-3,Ansamitocin P-3,Ansamitocin |Cas: 66547-09-9|Molecule Weight: 635.14|Molecule Formular: C32H43ClN2O9| Purity: >98%
Ansamitocin P-3, a potent anti-tumor maytansinoid found in Actinosynnema pretiosum, is a maytansine analog which displays potent cytotoxicity against the human solid tumor cell lines A-549 and HT-29.
in vitro: Linear calibration curves were obtained in the range 1-500 ng/mL using 0.2 mL rat plasma. The within-day coefficients of variation (CVs) were 12.9, 6.7, and 5.5% and the between-day CVs were 10.4, 6.5, and 6.4% (all n = 5) at 1, 10, and 200 ng/mL, respectively. Ansamitocin P-3 showed potent cytotoxicity against the human solid tumor cell lines A-549, HT-29.
in vivo: The major pathway of ansamitocin P-3 metabolism in human liver microsomes appears to be demethylation at C-10. The rate of metabolism of ansamitocin P-3 was different in rat and human liver microsomes. About 20% of ansamitocin P-3 was converted to its metabolites in rat liver microsomes and about 70% in human liver microsomes under the same conditions. Additionally, 10-O-demethylated ansamitocin P-3 was also detected in the urine after i.v. bolus administration of ansamitocin P-3 to Sprague-Dawley male rats.
For research and scientific purpose only, not for human use.
Ansamitocin P-3, a potent anti-tumor maytansinoid found in Actinosynnema pretiosum, is a maytansine analog which displays potent cytotoxicity against the human solid tumor cell lines A-549 and HT-29.
Product name: Ansamitocin P-3 |Cat No. DC8241|Other names: Ansamitocin P-3,Ansamitocin P-3,Ansamitocin |Cas: 66547-09-9|Molecule Weight: 635.14|Molecule Formular: C32H43ClN2O9| Purity: >98%
Ansamitocin P-3, a potent anti-tumor maytansinoid found in Actinosynnema pretiosum, is a maytansine analog which displays potent cytotoxicity against the human solid tumor cell lines A-549 and HT-29.
in vitro: Linear calibration curves were obtained in the range 1-500 ng/mL using 0.2 mL rat plasma. The within-day coefficients of variation (CVs) were 12.9, 6.7, and 5.5% and the between-day CVs were 10.4, 6.5, and 6.4% (all n = 5) at 1, 10, and 200 ng/mL, respectively. Ansamitocin P-3 showed potent cytotoxicity against the human solid tumor cell lines A-549, HT-29.
in vivo: The major pathway of ansamitocin P-3 metabolism in human liver microsomes appears to be demethylation at C-10. The rate of metabolism of ansamitocin P-3 was different in rat and human liver microsomes. About 20% of ansamitocin P-3 was converted to its metabolites in rat liver microsomes and about 70% in human liver microsomes under the same conditions. Additionally, 10-O-demethylated ansamitocin P-3 was also detected in the urine after i.v. bolus administration of ansamitocin P-3 to Sprague-Dawley male rats.
For research and scientific purpose only, not for human use.
MTS|For MTS assy|From DC Chemicals
MTS|For MTS assy|From DC Chemicals
MTS is water-soluble and used in the MTS assay.
Product name: MTS |Cat No. DC8240|Other names: MTS|Cas: 138169-43-4|Molecule Weight: 487.515|Molecule Formular: C20H17N5O6S2| Purity: >98%
MTS is water-soluble and used in the MTS assay.
For research and scientific purpose only, not for human use.
MTS is water-soluble and used in the MTS assay.
Product name: MTS |Cat No. DC8240|Other names: MTS|Cas: 138169-43-4|Molecule Weight: 487.515|Molecule Formular: C20H17N5O6S2| Purity: >98%
MTS is water-soluble and used in the MTS assay.
For research and scientific purpose only, not for human use.
SL 0101-1|Rsk inhibitor|DC Chemicals
SL 0101-1|Rsk inhibitor|DC Chemicals
SL 0101-1 is a selective inhibitor of p90 Rsk (ribosomal S6 kinase) (IC50 = 89 nM for Rsk-2).
Product name: SL 0101-1 |Cat No. DC8239|Other names: SL-0101-1,SL0101-1|Cas: 77307-50-7|Molecule Weight: 516.453|Molecule Formular: C25H24O12| Purity: >98%
SL 0101-1 is a selective inhibitor of p90 Rsk (ribosomal S6 kinase) (IC50 = 89 nM for Rsk-2). This product does not inhibit upstream kinases such as MEK, Raf and PKC. SL 0101-1 inhibits the growth of MCF-7 human breast cancer cells with no effect on the normal breast cell line.
For research and scientific purpose only, not for human use.
SL 0101-1 is a selective inhibitor of p90 Rsk (ribosomal S6 kinase) (IC50 = 89 nM for Rsk-2).
Product name: SL 0101-1 |Cat No. DC8239|Other names: SL-0101-1,SL0101-1|Cas: 77307-50-7|Molecule Weight: 516.453|Molecule Formular: C25H24O12| Purity: >98%
SL 0101-1 is a selective inhibitor of p90 Rsk (ribosomal S6 kinase) (IC50 = 89 nM for Rsk-2). This product does not inhibit upstream kinases such as MEK, Raf and PKC. SL 0101-1 inhibits the growth of MCF-7 human breast cancer cells with no effect on the normal breast cell line.
For research and scientific purpose only, not for human use.
Danoprevir (RG7227)|HCV NS3/4A inhibitor|DC Chemicals
Danoprevir (RG7227)|HCV NS3/4A inhibitor|DC Chemicals
Danoprevir is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A.
Product name: Danoprevir (RG7227) |Cat No. DC8238|Other names: Danoprevir, RG 7227|Cas: 850876-88-9|Molecule Weight: 731.83|Molecule Formular: C35H46FN5O9S| Purity: 0.95
Danoprevir(ITMN-191;R7227; RO5190591;RG7227) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A.
Danoprevir is an inhibitor of the NS3/4A protease.Danoprevir (ITMN 191; ITMN-191; R7227; RO5190591; RG7227)is useful for anti-HCV,anti-cancer. Danoprevir (0.29 nM) inhibits the reference genotype 1 NS3/4A protease half-maximally, but a high dose of Danoprevir (10 μM) shows no appreciably inhibition in a panel of 79 proteases, ion channels, transporters, and cell surface receptors. Danoprevir remains bound to and inhibits NS3/4A for more than 5 hours after its initial association. Danoprevir (45 nM) eliminates a patient-derived HCV genotype 1b replicon from hepatocyte-derived Huh7 cells with an EC50 of 1.8 nM. In HCV subgenomic replicon cell lines containing the individual mutations, V36M, R109K, and V170A substitutions confer little or no resistance to Danoprevir, but the R155K substitution confers a high level (62-fold increase) of resistance to Danoprevir. In Huh7.5 cells transfected with chimeric recombinant virus, Danoprevir shows antiviral inhibition effects against HCV genotypes 1, 4 and 6 with IC50 of 2-3 nM, which are >100-fold lower than genotypes 2/3/5 (280-750 nM).
For research and scientific purpose only, not for human use.
Danoprevir is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A.
Product name: Danoprevir (RG7227) |Cat No. DC8238|Other names: Danoprevir, RG 7227|Cas: 850876-88-9|Molecule Weight: 731.83|Molecule Formular: C35H46FN5O9S| Purity: 0.95
Danoprevir(ITMN-191;R7227; RO5190591;RG7227) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A.
Danoprevir is an inhibitor of the NS3/4A protease.Danoprevir (ITMN 191; ITMN-191; R7227; RO5190591; RG7227)is useful for anti-HCV,anti-cancer. Danoprevir (0.29 nM) inhibits the reference genotype 1 NS3/4A protease half-maximally, but a high dose of Danoprevir (10 μM) shows no appreciably inhibition in a panel of 79 proteases, ion channels, transporters, and cell surface receptors. Danoprevir remains bound to and inhibits NS3/4A for more than 5 hours after its initial association. Danoprevir (45 nM) eliminates a patient-derived HCV genotype 1b replicon from hepatocyte-derived Huh7 cells with an EC50 of 1.8 nM. In HCV subgenomic replicon cell lines containing the individual mutations, V36M, R109K, and V170A substitutions confer little or no resistance to Danoprevir, but the R155K substitution confers a high level (62-fold increase) of resistance to Danoprevir. In Huh7.5 cells transfected with chimeric recombinant virus, Danoprevir shows antiviral inhibition effects against HCV genotypes 1, 4 and 6 with IC50 of 2-3 nM, which are >100-fold lower than genotypes 2/3/5 (280-750 nM).
For research and scientific purpose only, not for human use.
LRRK2-IN-1|LRRK2 inhibitor|DC Chemicals
LRRK2-IN-1|LRRK2 inhibitor|DC Chemicals
LRRK2-IN-1 inhibits both wild-type and G2019S mutant LRRK2 kinase activity with IC50 values of 13 nM and 6 nM , respectively with 0.1 mM ATP in the assay.
Product name: LRRK2-IN-1 |Cat No. DC8237|Other names: LRRK2-IN-1, LRRK2 inhibitor|Cas: 1234480-84-2|Molecule Weight: 570.69|Molecule Formular: C31H38N8O3| Purity: >98%
Potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2). Inhibits both G2019S mutant and wild-type LRRK2 kinase activity (IC50 values are 6 and 13 nM respectively). Causes dephosphorylation, ubiquitination and degradation of LRRK2.
For research and scientific purpose only, not for human use.
LRRK2-IN-1 inhibits both wild-type and G2019S mutant LRRK2 kinase activity with IC50 values of 13 nM and 6 nM , respectively with 0.1 mM ATP in the assay.
Product name: LRRK2-IN-1 |Cat No. DC8237|Other names: LRRK2-IN-1, LRRK2 inhibitor|Cas: 1234480-84-2|Molecule Weight: 570.69|Molecule Formular: C31H38N8O3| Purity: >98%
Potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2). Inhibits both G2019S mutant and wild-type LRRK2 kinase activity (IC50 values are 6 and 13 nM respectively). Causes dephosphorylation, ubiquitination and degradation of LRRK2.
For research and scientific purpose only, not for human use.
Repinotan (BAYx3702)|5HT1A-receptor inhibitor|DC Chemicals
Repinotan (BAYx3702)|5HT1A-receptor inhibitor|DC Chemicals
Repinotan is a high-affinity, selective, full agonist of the 5HT1A-receptor subtype with neuroprotective properties.
Product name: Repinotan (BAYx3702) |Cat No. DC8235|Other names: Repinotan, BAYx3702|Cas: 144980-29-0|Molecule Weight: 400.49|Molecule Formular: C21H24N2O4S| Purity: >98%
Repinotan is a high-affinity, selective, full agonist of the 5HT1A-receptor subtype with neuroprotective properties.
For research and scientific purpose only, not for human use.
Repinotan is a high-affinity, selective, full agonist of the 5HT1A-receptor subtype with neuroprotective properties.
Product name: Repinotan (BAYx3702) |Cat No. DC8235|Other names: Repinotan, BAYx3702|Cas: 144980-29-0|Molecule Weight: 400.49|Molecule Formular: C21H24N2O4S| Purity: >98%
Repinotan is a high-affinity, selective, full agonist of the 5HT1A-receptor subtype with neuroprotective properties.
For research and scientific purpose only, not for human use.
PNRI-299(PNRI299)|AP-1 inhibitor|DC Chemicals
PNRI-299(PNRI299)|AP-1 inhibitor|DC Chemicals
PNRI-299 is an inhibitor of activator protein-1 (AP-1) transcription (IC(50) of 20 microM) without affecting NF-kappaB transcription (up to 200 microM) or thioredoxin (up to 200 microM).
Product name: PNRI-299 |Cat No. DC8234|Other names: PNRI299,PNRI-299,PNRI 299|Cas: 550368-41-7|Molecule Weight: 401.37|Molecule Formular: C21H15N5O4| Purity: >98%
PNRI-299, was identified that selectively inhibited AP-1 transcription (IC(50) of 20 microM) without affecting NF-kappaB transcription (up to 200 microM) or thioredoxin (up to 200 microM). The molecular target of PNRI-299 was determined to be the oxidoreductase, redox effector factor-1 by an affinity chromatography approach. The selective redox effector factor-1 inhibitor, PNRI-299, significantly reduced airway eosinophil infiltration, mucus hypersecretion, edema, and IL-4 levels in a mouse asthma model. These data validate AP-1 as an important therapeutic target in allergic airway inflammation.
For research and scientific purpose only, not for human use.
PNRI-299 is an inhibitor of activator protein-1 (AP-1) transcription (IC(50) of 20 microM) without affecting NF-kappaB transcription (up to 200 microM) or thioredoxin (up to 200 microM).
Product name: PNRI-299 |Cat No. DC8234|Other names: PNRI299,PNRI-299,PNRI 299|Cas: 550368-41-7|Molecule Weight: 401.37|Molecule Formular: C21H15N5O4| Purity: >98%
PNRI-299, was identified that selectively inhibited AP-1 transcription (IC(50) of 20 microM) without affecting NF-kappaB transcription (up to 200 microM) or thioredoxin (up to 200 microM). The molecular target of PNRI-299 was determined to be the oxidoreductase, redox effector factor-1 by an affinity chromatography approach. The selective redox effector factor-1 inhibitor, PNRI-299, significantly reduced airway eosinophil infiltration, mucus hypersecretion, edema, and IL-4 levels in a mouse asthma model. These data validate AP-1 as an important therapeutic target in allergic airway inflammation.
For research and scientific purpose only, not for human use.
ZK261991（ZK991）|DC Chemicals
ZK261991（ZK991）|DC Chemicals
ZK261991 is a highly selective and potent VEGFR-kinase inhibitor, which is orally available.
Product name: ZK261991(ZK991) |Cat No. DC8233|Other names: ZK-261991，ZK 261991，ZK-991，ZK 991|Cas: 886563-25-3|Molecule Weight: 443.5|Molecule Formular: C24H25N7O2| Purity: >98%
ZK261991 is a highly selective and potent VEGFR-kinase inhibitor, which is orally available. Kaplan-Meier analysis of survival showed a significant benefit for mice treated with ZK261991 after HPAF-2 tumor resection: 83.8 days (95% CI 73.9-93.6) vs. 60.9 days (95% CI 48.9-73.0), p = 0.006. Adjuvant treatment with ZK261991 of AsPC-1-derived tumors showed a tendency towards a benefit compared to control but no significant difference: 75.8 days (95% CI 59.7-91.9) vs. 65.7 days (95% CI 51.6-79.7). There were no significant differences in dissemination score and size of recurrent tumor mass between the treatment groups. Adjuvant anti-angiogenic therapy with the novel VEGFR-inhibitor ZK261991 resulted in a significant survival benefit after curative tumor resection in a clinically relevant orthotopic animal model of pancreatic cancer. Combination of anti-angiogenic treatment with cytotoxic agents may further improve the results of adjuvant therapy.
For research and scientific purpose only, not for human use.
ZK261991 is a highly selective and potent VEGFR-kinase inhibitor, which is orally available.
Product name: ZK261991(ZK991) |Cat No. DC8233|Other names: ZK-261991，ZK 261991，ZK-991，ZK 991|Cas: 886563-25-3|Molecule Weight: 443.5|Molecule Formular: C24H25N7O2| Purity: >98%
ZK261991 is a highly selective and potent VEGFR-kinase inhibitor, which is orally available. Kaplan-Meier analysis of survival showed a significant benefit for mice treated with ZK261991 after HPAF-2 tumor resection: 83.8 days (95% CI 73.9-93.6) vs. 60.9 days (95% CI 48.9-73.0), p = 0.006. Adjuvant treatment with ZK261991 of AsPC-1-derived tumors showed a tendency towards a benefit compared to control but no significant difference: 75.8 days (95% CI 59.7-91.9) vs. 65.7 days (95% CI 51.6-79.7). There were no significant differences in dissemination score and size of recurrent tumor mass between the treatment groups. Adjuvant anti-angiogenic therapy with the novel VEGFR-inhibitor ZK261991 resulted in a significant survival benefit after curative tumor resection in a clinically relevant orthotopic animal model of pancreatic cancer. Combination of anti-angiogenic treatment with cytotoxic agents may further improve the results of adjuvant therapy.
For research and scientific purpose only, not for human use.
AZD5582，AZD 5582|IAP inhibitor|DC Chemicals
AZD5582，AZD 5582|IAP inhibitor|DC Chemicals
AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively).
Product name: AZD 5582 |Cat No. DC8232|Other names: AZD5582，AZD-5582，AZD 5582|Cas: 1258392-53-8|Molecule Weight: 1015.29|Molecule Formular: C58H78N8O8| Purity: >98%
AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively).
AZD5582 causes cIAP1 degradation and induces apoptosis in the MDA-MB-231 breast cancer cell line at subnanomolar concentrations in vitro. When administered intravenously to MDA-MB-231 xenograft-bearing mice, AZD5582 results in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg. Antiproliferative effects are observed with AZD5582 in only a small subset of the over 200 cancer cell lines examined, consistent with other published IAP inhibitors. AZD5582 significantly enhanced apoptosis induced by the death receptor (DR) agonist tumour necrosis factor-related apoptosis-inducing ligand (TRAIL). Importantly, killing by TRAIL plus AZD5582 was independent of adverse prognostic features including TP53 deletion which is strongly associated with chemoresistance in CLL.
For research and scientific purpose only, not for human use.
AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively).
Product name: AZD 5582 |Cat No. DC8232|Other names: AZD5582，AZD-5582，AZD 5582|Cas: 1258392-53-8|Molecule Weight: 1015.29|Molecule Formular: C58H78N8O8| Purity: >98%
AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively).
AZD5582 causes cIAP1 degradation and induces apoptosis in the MDA-MB-231 breast cancer cell line at subnanomolar concentrations in vitro. When administered intravenously to MDA-MB-231 xenograft-bearing mice, AZD5582 results in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg. Antiproliferative effects are observed with AZD5582 in only a small subset of the over 200 cancer cell lines examined, consistent with other published IAP inhibitors. AZD5582 significantly enhanced apoptosis induced by the death receptor (DR) agonist tumour necrosis factor-related apoptosis-inducing ligand (TRAIL). Importantly, killing by TRAIL plus AZD5582 was independent of adverse prognostic features including TP53 deletion which is strongly associated with chemoresistance in CLL.
For research and scientific purpose only, not for human use.
LDN-192960|LDN192960，haspin inhibitor|From DC Chemicals
LDN-192960|LDN192960，haspin inhibitor|From DC Chemicals
LDN-192960 is a potent and selective inhibitor of haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase). IC50 = 0.010 µm
Product name: LDN-192960 2HCl |Cat No. DC8231|Other names: LDN-192960,LDN192960|Cas: 184582-62-5|Molecule Weight: 401.35|Molecule Formular: C18H20N2O2S · 2HCl | Purity: >98%
LDN-192960 is a potent and selective inhibitor of haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase). IC50 = 0.010 µm
For research and scientific purpose only, not for human use.
LDN-192960 is a potent and selective inhibitor of haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase). IC50 = 0.010 µm
Product name: LDN-192960 2HCl |Cat No. DC8231|Other names: LDN-192960,LDN192960|Cas: 184582-62-5|Molecule Weight: 401.35|Molecule Formular: C18H20N2O2S · 2HCl | Purity: >98%
LDN-192960 is a potent and selective inhibitor of haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase). IC50 = 0.010 µm
For research and scientific purpose only, not for human use.
FLT3-IN-1|Flt3 inhibitor|DC Chemicals
FLT3-IN-1|Flt3 inhibitor|DC Chemicals
FLT3-IN-1 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.
Product name: FLT3-IN-1 |Cat No. DC8230|Other names: FLT3-IN-1|Cas: 1370256-78-2|Molecule Weight: 537.66|Molecule Formular: C25H27N7O3S2| Purity: >98%
FLT3-IN-1 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.
in vitro: FLT3-IN-1 inhibited FLT3 phosphorylation in a dose-dependent manner. Consistent with the downregulation of the phosphorylation of FLT3, the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 was also significantly inhibited at concentrations >0.1 μM. FLT3-IN-1 potently inhibited the growth of MV4-11 cells that express FLT3-ITD, with an IC50 value of 0.006 μM. It just exhibited very weak inhibitory activity against human T lymphoma Jurkat cells, human Burkitt’s lymphoma Ramos cells, human lung cancer PC-9 and H292 cells, and human epithelial carcinoma A431 cells (IC50: 3.05 μM, 6.25 μM, 3.72 μM, 6.94 μM, and 8.91 μM, respectively). For other leukemia and solid tumor cell lines, including K562, U937, Karpas299, HCC827, A549, H2228, H820, MDA-MB-231, BT474, MCF-7, HCT116, SW480, LoVo, HeLa, SKOV-3, SK, DU145, PC-3, A431, and SH-SY5Y.
in vivo: Treatment with FLT3-IN-1 at 100 mg/kg/d resulted in rapid and complete tumor regression in all mice of this group. FLT3-IN-1 treatment at 20 mg/kg/d and 40 mg/kg/d significantly slowed down the tumor growth; the tumor inhibition rates are 66% and 84%, respectively. Moreover, during the whole experiment, no significant weight loss or any other obvious signs of toxicity were observed for all of the FLT3-IN-1-treated mice.
For research and scientific purpose only, not for human use.
FLT3-IN-1 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.
Product name: FLT3-IN-1 |Cat No. DC8230|Other names: FLT3-IN-1|Cas: 1370256-78-2|Molecule Weight: 537.66|Molecule Formular: C25H27N7O3S2| Purity: >98%
FLT3-IN-1 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.
in vitro: FLT3-IN-1 inhibited FLT3 phosphorylation in a dose-dependent manner. Consistent with the downregulation of the phosphorylation of FLT3, the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 was also significantly inhibited at concentrations >0.1 μM. FLT3-IN-1 potently inhibited the growth of MV4-11 cells that express FLT3-ITD, with an IC50 value of 0.006 μM. It just exhibited very weak inhibitory activity against human T lymphoma Jurkat cells, human Burkitt’s lymphoma Ramos cells, human lung cancer PC-9 and H292 cells, and human epithelial carcinoma A431 cells (IC50: 3.05 μM, 6.25 μM, 3.72 μM, 6.94 μM, and 8.91 μM, respectively). For other leukemia and solid tumor cell lines, including K562, U937, Karpas299, HCC827, A549, H2228, H820, MDA-MB-231, BT474, MCF-7, HCT116, SW480, LoVo, HeLa, SKOV-3, SK, DU145, PC-3, A431, and SH-SY5Y.
in vivo: Treatment with FLT3-IN-1 at 100 mg/kg/d resulted in rapid and complete tumor regression in all mice of this group. FLT3-IN-1 treatment at 20 mg/kg/d and 40 mg/kg/d significantly slowed down the tumor growth; the tumor inhibition rates are 66% and 84%, respectively. Moreover, during the whole experiment, no significant weight loss or any other obvious signs of toxicity were observed for all of the FLT3-IN-1-treated mice.
For research and scientific purpose only, not for human use.
Vorapaxar Sulfate (SCH 530348)|From DC Chemicals
Vorapaxar Sulfate (SCH 530348)|From DC Chemicals
Vorapaxar is an antagonist of the protease activated receptor-1 (PAR-1), the principal platelet thrombin receptor.
Product name: Vorapaxar Sulfate (SCH 530348) |Cat No. DC8229|Other names: Vorapaxar， SCH 530348|Cas: 705260-08-8|Molecule Weight: 590.66|Molecule Formular: C29H35FN2O8S| Purity: >98%
Vorapaxar is an antagonist of the protease activated receptor-1 (PAR-1), the principal platelet thrombin receptor.
For research and scientific purpose only, not for human use.
Vorapaxar is an antagonist of the protease activated receptor-1 (PAR-1), the principal platelet thrombin receptor.
Product name: Vorapaxar Sulfate (SCH 530348) |Cat No. DC8229|Other names: Vorapaxar， SCH 530348|Cas: 705260-08-8|Molecule Weight: 590.66|Molecule Formular: C29H35FN2O8S| Purity: >98%
Vorapaxar is an antagonist of the protease activated receptor-1 (PAR-1), the principal platelet thrombin receptor.
For research and scientific purpose only, not for human use.
AZD-8186|AZD8186|PI3K/δ inhibitor|DC Chemicals
AZD-8186|AZD8186|PI3K/δ inhibitor|DC Chemicals
AZD8186 is an inhibitor of PI3Kβ and PI3Kδ.
Product name: AZD8186 |Cat No. DC8228|Other names: AZD-8186，AZD 8186|Cas: 1296270-45-5|Molecule Weight: 457.47
|Molecule Formular: C24H25F2N3O4| Purity: >98%
In vitro, AZD8186 inhibited growth of a range of cell lines. Sensitivity was associated with inhibition of the AKT pathway. Cells sensitive to AZD8186 (GI50 < 1 μmol/L) are enriched for, but not exclusively associated with, PTEN deficiency. In vivo, AZD8186 inhibits PI3K pathway biomarkers in prostate and TNBC tumors. Scheduling treatment with AZD8186 shows antitumor activity required only intermittent exposure, and that increased tumor control is achieved when AZD8186 is used in combination with docetaxel. AZD8186 is a potent inhibitor of PI3Kβ with activity against PI3Kδ signaling, and has potential to reduce growth of tumors dependent on dysregulated PTEN for growth. Moreover, AZD8186 can be combined with docetaxel, a chemotherapy commonly used to treat advanced TBNC and prostate tumors. The ability to schedule AZD8186 and maintain efficacy offers opportunity to combine AZD8186 more effectively with other drugs.
For research and scientific purpose only, not for human use.
AZD8186 is an inhibitor of PI3Kβ and PI3Kδ.
Product name: AZD8186 |Cat No. DC8228|Other names: AZD-8186，AZD 8186|Cas: 1296270-45-5|Molecule Weight: 457.47
|Molecule Formular: C24H25F2N3O4| Purity: >98%
In vitro, AZD8186 inhibited growth of a range of cell lines. Sensitivity was associated with inhibition of the AKT pathway. Cells sensitive to AZD8186 (GI50 < 1 μmol/L) are enriched for, but not exclusively associated with, PTEN deficiency. In vivo, AZD8186 inhibits PI3K pathway biomarkers in prostate and TNBC tumors. Scheduling treatment with AZD8186 shows antitumor activity required only intermittent exposure, and that increased tumor control is achieved when AZD8186 is used in combination with docetaxel. AZD8186 is a potent inhibitor of PI3Kβ with activity against PI3Kδ signaling, and has potential to reduce growth of tumors dependent on dysregulated PTEN for growth. Moreover, AZD8186 can be combined with docetaxel, a chemotherapy commonly used to treat advanced TBNC and prostate tumors. The ability to schedule AZD8186 and maintain efficacy offers opportunity to combine AZD8186 more effectively with other drugs.
For research and scientific purpose only, not for human use.
SA4503|SA 4503|sigma 1 receptor agonist|DC Chemicals
SA4503|SA 4503|sigma 1 receptor agonist|DC Chemicals
SA4503 is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity for the sigma 2 receptor.
Product name: SA4503 2HCl |Cat No. DC8227|Other names: SA 4503,SA-4503|Cas: 165377-44-6|Molecule Weight: 441.43|Molecule Formular: C23H34Cl2N2O2| Purity: >98%
in vitro: SA4503 showed little affinity for 36 other receptors, ion channels and second messenger systems. SA4503 significantly increased the KD value, but did not affect the Bmax value for specific (+)-[3H]pentazocine binding. SA4503 is a potent and selective agonist for the sigma 1 receptor subtype in the brain. At concentrations of 1-10μM, SA4503 reduced SOD1(G93A)-induced cell death in a concentration-dependent manner.
in vivo: The intravenous administration of SA4503 (0.01-1.28 mg/kg) did not significantly alter the firing rate or pattern of spontaneously active DA neurons in either the SNC or VTA. A single injection of either 0.1 or 0.3 mg/kg i.p. of SA4503 did not alter the number of spontaneously active SNC and VTA DA neurons. In contrast, a single injection of 1 mg/kg i.p. of SA4503 produced a significant decrease and increase in the number of spontaneously active SNC and VTA DA neurons, respectively. SA4503 suppressed the progression of ALS in an SOD1(G93A) ALS mouse model. SA4503 did not affect the onset time of ALS. However, it significantly extended the survival time in the SOD1(G93A) mice compared with a vehicle-treated group.
For research and scientific purpose only, not for human use.
SA4503 is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity for the sigma 2 receptor.
Product name: SA4503 2HCl |Cat No. DC8227|Other names: SA 4503,SA-4503|Cas: 165377-44-6|Molecule Weight: 441.43|Molecule Formular: C23H34Cl2N2O2| Purity: >98%
in vitro: SA4503 showed little affinity for 36 other receptors, ion channels and second messenger systems. SA4503 significantly increased the KD value, but did not affect the Bmax value for specific (+)-[3H]pentazocine binding. SA4503 is a potent and selective agonist for the sigma 1 receptor subtype in the brain. At concentrations of 1-10μM, SA4503 reduced SOD1(G93A)-induced cell death in a concentration-dependent manner.
in vivo: The intravenous administration of SA4503 (0.01-1.28 mg/kg) did not significantly alter the firing rate or pattern of spontaneously active DA neurons in either the SNC or VTA. A single injection of either 0.1 or 0.3 mg/kg i.p. of SA4503 did not alter the number of spontaneously active SNC and VTA DA neurons. In contrast, a single injection of 1 mg/kg i.p. of SA4503 produced a significant decrease and increase in the number of spontaneously active SNC and VTA DA neurons, respectively. SA4503 suppressed the progression of ALS in an SOD1(G93A) ALS mouse model. SA4503 did not affect the onset time of ALS. However, it significantly extended the survival time in the SOD1(G93A) mice compared with a vehicle-treated group.
For research and scientific purpose only, not for human use.
RI-2|RI2|RAD51 inhibitor|DC Chemicals
RI-2|RI2|RAD51 inhibitor|DC Chemicals
RI-2 is an optimized RAD51 inhibitor with an IC50 of 44.17 μM in the standard DNA binding assay; specifically inhibits HR(Homologous recombination) repair in human cells.
Product name: RI-2 |Cat No. DC8226|Other names: RI2,RI 2|Cas: 1417162-36-7|Molecule Weight: 433.28|Molecule Formular: C21H18Cl2N2O4| Purity: >98%
RI-2 is an optimized RAD51 inhibitor with an IC50 of 44.17 μM in the standard DNA binding assay; specifically inhibits HR(Homologous recombination) repair in human cells. RI-2 appears to bind reversibly to the same site on the RAD51 protein as does RI-1. Like RI-1, RI-2 specifically inhibits HR repair in human cells.
For research and scientific purpose only, not for human use.
RI-2 is an optimized RAD51 inhibitor with an IC50 of 44.17 μM in the standard DNA binding assay; specifically inhibits HR(Homologous recombination) repair in human cells.
Product name: RI-2 |Cat No. DC8226|Other names: RI2,RI 2|Cas: 1417162-36-7|Molecule Weight: 433.28|Molecule Formular: C21H18Cl2N2O4| Purity: >98%
RI-2 is an optimized RAD51 inhibitor with an IC50 of 44.17 μM in the standard DNA binding assay; specifically inhibits HR(Homologous recombination) repair in human cells. RI-2 appears to bind reversibly to the same site on the RAD51 protein as does RI-1. Like RI-1, RI-2 specifically inhibits HR repair in human cells.
For research and scientific purpose only, not for human use.
SAG|Smoothened (Smo) receptor agonist|DC Chemicasl
SAG|Smoothened (Smo) receptor agonist|DC Chemicasl
SAG is a potent Smoothened (Smo) receptor agonist (Kd = 59 nM); potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM).
Product name: SAG |Cat No. DC8225|Other names: SAG,912545-86-9|Cas: 912545-86-9|Molecule Weight: 490.06|Molecule Formular: C28H28ClN3OS| Purity: >98%
The binding of BODIPY-cyclopamine to the Smo-deletion mutants was inhibited by 150 nM SAG to an extent similar to that observed with cells expressing WT Smo. SAG may interact not only with Smo, but also with a cellular effector of Smo activation, thereby inducing Hh pathway activation by facilitating the association of these two proteins at optimal SAG concentrations.
For research and scientific purpose only, not for human use.
SAG is a potent Smoothened (Smo) receptor agonist (Kd = 59 nM); potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM).
Product name: SAG |Cat No. DC8225|Other names: SAG,912545-86-9|Cas: 912545-86-9|Molecule Weight: 490.06|Molecule Formular: C28H28ClN3OS| Purity: >98%
The binding of BODIPY-cyclopamine to the Smo-deletion mutants was inhibited by 150 nM SAG to an extent similar to that observed with cells expressing WT Smo. SAG may interact not only with Smo, but also with a cellular effector of Smo activation, thereby inducing Hh pathway activation by facilitating the association of these two proteins at optimal SAG concentrations.
For research and scientific purpose only, not for human use.
Lifitegrast(SAR 1118)|LFA-1/ICAM-1 antagonist|DC Chemicals
Lifitegrast(SAR 1118)|LFA-1/ICAM-1 antagonist|DC Chemicals
SAR 1118 is a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist for treating dry eye.
Product name: Lifitegrast(SAR 1118) |Cat No. DC8224|Other names: Lifitegrast,SAR1118|Cas: 1025967-78-5|Molecule Weight: 615.49|Molecule Formular: C29H24CL2N2O7S| Purity: >98%
SAR 1118 is a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist for treating dry eye.
For research and scientific purpose only, not for human use.
SAR 1118 is a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist for treating dry eye.
Product name: Lifitegrast(SAR 1118) |Cat No. DC8224|Other names: Lifitegrast,SAR1118|Cas: 1025967-78-5|Molecule Weight: 615.49|Molecule Formular: C29H24CL2N2O7S| Purity: >98%
SAR 1118 is a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist for treating dry eye.
For research and scientific purpose only, not for human use.
TP-0903|Axl kinase inhibitor|DC Chemicals
TP-0903|Axl kinase inhibitor|DC Chemicals
TP-0903 is a a high-affinity Axl inhibitor with IC50 of 27 nM.
Product name: TP-0903 |Cat No. DC8223|Other names: TP-0903 ,TP0903 , TP-0903 |Cas: 1341200-45-0|Molecule Weight: 516.06|Molecule Formular: C24H30ClN7O2S| Purity: >98%
TP-0903 induces massive apoptosis in CLL B cells with LD50 values of nanomolar ranges. Importantly, CLL BMSCs could not protect the leukemic B cells from TP-0903-induced apoptosis. A marked reduction of the antiapoptotic proteins Mcl-1, Bcl-2, and XIAP and upregulation of the proapoptotic protein BIM in CLL B cells was detected as a result of Axl inhibition. Finally, combination of TP-0903 with BTK inhibitors augments CLL B-cell apoptosis.Administration of TP-0903 either as a single agent or in combination with BTK inhibitors may be effective in treating patients with CLL.
For research and scientific purpose only, not for human use.
TP-0903 is a a high-affinity Axl inhibitor with IC50 of 27 nM.
Product name: TP-0903 |Cat No. DC8223|Other names: TP-0903 ,TP0903 , TP-0903 |Cas: 1341200-45-0|Molecule Weight: 516.06|Molecule Formular: C24H30ClN7O2S| Purity: >98%
TP-0903 induces massive apoptosis in CLL B cells with LD50 values of nanomolar ranges. Importantly, CLL BMSCs could not protect the leukemic B cells from TP-0903-induced apoptosis. A marked reduction of the antiapoptotic proteins Mcl-1, Bcl-2, and XIAP and upregulation of the proapoptotic protein BIM in CLL B cells was detected as a result of Axl inhibition. Finally, combination of TP-0903 with BTK inhibitors augments CLL B-cell apoptosis.Administration of TP-0903 either as a single agent or in combination with BTK inhibitors may be effective in treating patients with CLL.
For research and scientific purpose only, not for human use.
G007-LK|tankyrases 1/2 inhibitor|DC Chemicals
G007-LK|tankyrases 1/2 inhibitor|DC Chemicals
G007-LK is a potent, "rule of 5" compliant and a metabolically stable TNKS1/2 inhibitor.
Product name: G007-LK |Cat No. DC8222|Other names: G007-LK ,G007-LK,G007-LK |Cas: 1380672-07-0|Molecule Weight: 529.07|Molecule Formular: C25H16ClN7O3S| Purity: >98%
G007-LK is a potent, "rule of 5" compliant and a metabolically stable TNKS1/2 inhibitor. G007-LK displayed high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM, respectively, and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice.
For research and scientific purpose only, not for human use.
G007-LK is a potent, "rule of 5" compliant and a metabolically stable TNKS1/2 inhibitor.
Product name: G007-LK |Cat No. DC8222|Other names: G007-LK ,G007-LK,G007-LK |Cas: 1380672-07-0|Molecule Weight: 529.07|Molecule Formular: C25H16ClN7O3S| Purity: >98%
G007-LK is a potent, "rule of 5" compliant and a metabolically stable TNKS1/2 inhibitor. G007-LK displayed high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM, respectively, and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice.
For research and scientific purpose only, not for human use.
NVP-QAV680|CRTh2 receptor antagonist|DC Chemicals
NVP-QAV680|CRTh2 receptor antagonist|DC Chemicals
NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with Ki of 36 nM by 3H-PGD2 filtration binding assay.
Product name: NVP-QAV680 |Cat No. DC8221|Other names: NVP-QAV680,NVPQAV680|Cas: 872365-16-7|Molecule Weight: 358.41|Molecule Formular: C18H18N2O4S| Purity: >98%
NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with Ki of 36 nM by 3H-PGD2 filtration binding assay.
NVP-QAV680 is a highly selective compound with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development.
in vitro: NVP-QAV680 was found to be inactive against eotaxin stimulated shape change mediated through the CCR-3 receptor. NVP-QAV680 elicited a potent inhibitory response to shape change elicited by both PGD2 and DK-PGD2 in whole blood. NVP-QAV680 exhibited nM potency for the blockade of DK-PGD2 induced IL-5 and IL-13 cytokine production from primary cultured human CD4+ Th2 lymphocytes.
in vivo: NVP-QAV680 dosed orally in an adapted variant of this model showed statistically significant inhibition of eosinophil infiltration after bronchoalveolar lavage (BAL) at a minimum dose of 1 mg/kg, with a trend to dose-dependency, thus confirming CRTh2 target engagement with a readout in a disease relevant tissue. In a follow up experiment, NVP-QAV680 was applied at lower doses of 0.3 and 0.1 mg/kg, with plasma sampling concomitant with BAL determination.
For research and scientific purpose only, not for human use.
NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with Ki of 36 nM by 3H-PGD2 filtration binding assay.
Product name: NVP-QAV680 |Cat No. DC8221|Other names: NVP-QAV680,NVPQAV680|Cas: 872365-16-7|Molecule Weight: 358.41|Molecule Formular: C18H18N2O4S| Purity: >98%
NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with Ki of 36 nM by 3H-PGD2 filtration binding assay.
NVP-QAV680 is a highly selective compound with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development.
in vitro: NVP-QAV680 was found to be inactive against eotaxin stimulated shape change mediated through the CCR-3 receptor. NVP-QAV680 elicited a potent inhibitory response to shape change elicited by both PGD2 and DK-PGD2 in whole blood. NVP-QAV680 exhibited nM potency for the blockade of DK-PGD2 induced IL-5 and IL-13 cytokine production from primary cultured human CD4+ Th2 lymphocytes.
in vivo: NVP-QAV680 dosed orally in an adapted variant of this model showed statistically significant inhibition of eosinophil infiltration after bronchoalveolar lavage (BAL) at a minimum dose of 1 mg/kg, with a trend to dose-dependency, thus confirming CRTh2 target engagement with a readout in a disease relevant tissue. In a follow up experiment, NVP-QAV680 was applied at lower doses of 0.3 and 0.1 mg/kg, with plasma sampling concomitant with BAL determination.
For research and scientific purpose only, not for human use.
GSK2578999(GSK8999)|HIV-1 maturation inhibitor
GSK2578999(GSK8999)|HIV-1 maturation inhibitor|DC Chemicals
GSK2578999 is an HIV-1 maturation inhibitor with an improved virology profile against gag polymorphisms.
Product name: GSK2578999(GSK8999) |Cat No. DC8219|Other names: GSK257899,GSK8899|Cas: 1422355-59-6|Molecule Weight: 776.44|Molecule Formular: C46H62ClNO7| Purity: >98%
GSK2578999 is an HIV-1 maturation inhibitor with an improved virology profile against gag polymorphisms.
For research and scientific purpose only, not for human use.
GSK2578999 is an HIV-1 maturation inhibitor with an improved virology profile against gag polymorphisms.
Product name: GSK2578999(GSK8999) |Cat No. DC8219|Other names: GSK257899,GSK8899|Cas: 1422355-59-6|Molecule Weight: 776.44|Molecule Formular: C46H62ClNO7| Purity: >98%
GSK2578999 is an HIV-1 maturation inhibitor with an improved virology profile against gag polymorphisms.
For research and scientific purpose only, not for human use.
YO-01027(Dibenzazepine)|γ secretase inhibitor|DC Chemicals
YO-01027(Dibenzazepine)|γ secretase inhibitor|DC Chemicals
YO-01027 (Dibenzazepine, DBZ) is a dipeptidic g-secretase inhibitor with IC50 of 2.6 and 2.9 nM for APPL and Notch, respectively.
Product name: YO-01027(Dibenzazepine) |Cat No. DC8217|Other names: YO-01027(Dibenzazepine) |Cas: 209984-56-5|Molecule Weight: 463.48|Molecule Formular: C26H23F2N3O3| Purity: >98%
YO-01027 (Dibenzazepine, DBZ) is a dipeptidic g-secretase inhibitor with IC50 of 2.6 and 2.9 nM for APPL and Notch, respectively. YO-01027 targets the Presenilin fragment. Increasing concentrations of YO-01027 administered to APPl- or Notch-expressing cells leads to the progressive accumulation of APPL C-terminal fragments and a decrease in NICD production in a dose-dependent manner.
In an in vitro model of human corneal and conjunctival epithelial cell differentation, YO-01027 impaired MUC16 biosynthesis in a concentration-dependent manner.
In oncology models, YO-01027 preferentially inhibited Notch and significantly decreased MCF7 tumors and increased latency compared with control mice.
For research and scientific purpose only, not for human use.
YO-01027 (Dibenzazepine, DBZ) is a dipeptidic g-secretase inhibitor with IC50 of 2.6 and 2.9 nM for APPL and Notch, respectively.
Product name: YO-01027(Dibenzazepine) |Cat No. DC8217|Other names: YO-01027(Dibenzazepine) |Cas: 209984-56-5|Molecule Weight: 463.48|Molecule Formular: C26H23F2N3O3| Purity: >98%
YO-01027 (Dibenzazepine, DBZ) is a dipeptidic g-secretase inhibitor with IC50 of 2.6 and 2.9 nM for APPL and Notch, respectively. YO-01027 targets the Presenilin fragment. Increasing concentrations of YO-01027 administered to APPl- or Notch-expressing cells leads to the progressive accumulation of APPL C-terminal fragments and a decrease in NICD production in a dose-dependent manner.
In an in vitro model of human corneal and conjunctival epithelial cell differentation, YO-01027 impaired MUC16 biosynthesis in a concentration-dependent manner.
In oncology models, YO-01027 preferentially inhibited Notch and significantly decreased MCF7 tumors and increased latency compared with control mice.
For research and scientific purpose only, not for human use.
GDC-0349| mTOR inhibitor|DC Chemicals
GDC-0349| mTOR inhibitor|DC Chemicals
GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM; >700-fold selectivity over PI3Kα and other 266 kinases.
Product name: GDC-0349 |Cat No. DC8216|Other names: GDC-0349|Cas: 1207360-89-1|Molecule Weight: 452.54928|Molecule Formular: C24H32N6O3| Purity: >98%
GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM; >700-fold selectivity over PI3Kα and other 266 kinases.GDC-0349 has remarkable selectivity over 266 kinases, including all isoforms of PI3K. GDC-0349 inhibits downstream markers of mTOR, including phospho-4EBP1 and phospho-Akt(S473) in an in vivo PK/PD study in mouse, consistent with an inhibition of both mTORC1 and mTORC2 complexes. GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models. When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 inhibits tumor growth in a dose-dependent manner. It is also efficacious in other xenograft models, including PC3 (PTEN null) and 786-O (VHL mutant).
For research and scientific purpose only, not for human use.
GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM; >700-fold selectivity over PI3Kα and other 266 kinases.
Product name: GDC-0349 |Cat No. DC8216|Other names: GDC-0349|Cas: 1207360-89-1|Molecule Weight: 452.54928|Molecule Formular: C24H32N6O3| Purity: >98%
GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM; >700-fold selectivity over PI3Kα and other 266 kinases.GDC-0349 has remarkable selectivity over 266 kinases, including all isoforms of PI3K. GDC-0349 inhibits downstream markers of mTOR, including phospho-4EBP1 and phospho-Akt(S473) in an in vivo PK/PD study in mouse, consistent with an inhibition of both mTORC1 and mTORC2 complexes. GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models. When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 inhibits tumor growth in a dose-dependent manner. It is also efficacious in other xenograft models, including PC3 (PTEN null) and 786-O (VHL mutant).
For research and scientific purpose only, not for human use.
RO4929097|γ secretase inhibitor|DC Chemicals
RO4929097|γ secretase inhibitor|DC Chemicals
RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.
Product name: RO4929097 |Cat No. DC8215|Other names: RO4929097|Cas: 847925-91-1|Molecule Weight: 469.4|Molecule Formular: C22H20F5N3O3| Purity: >98%
RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.in vitro: RO4929097 decreases the amount of Aβ peptides secreted into the culture medium in HEK293 cells with EC50 of 14 nM. RO4929097 strongly inhibits Notch processing with EC50 of 5 nM in the Notch cell-based reporter assay. The potency of RO4929097 in cell-free and cellular assays is in the low nanomolar range with >100-fold selectivity observed with respect to 75 other proteins of various types including receptors, ion channels, and enzymes (CEREP panel). After 5 days of treatment, RO4929097 reduces the production of ICN in the human NSCLC A549 cells inducing a flattened and less transformed tumor cell phenotype in tissue culture . RO4929097 blocks Notch processing in human non-small cell lung carcinoma cells and decreases expression of the Notch transcriptional target gene Hes1. Treatment with RO4929097 reveals a two- to threefold decrease in the expression of direct Notch target genes, Hes1, Hey1, and Heyl in SUM149 and a 3.5- to eightfold decrease in expression in SUM190 cells. RO4929097 modestly inhibits the growth of SUM149 cells in a dose-dependent manner. At a concentration of 1 μM of RO4929097, growth inhibition is 20 % for SUM149 and 10 % for SUM190 cells, relative to vehicle-treated controls. RO4929097 decreases the production of inflammatory cytokines by T-cells. Furthermore, with RO4929097 treatment, there is a shift in favor of TH2 over TH1 cytokines. In addition, T-cell activation induced IL-6 production would be increased with RO4929097. Upon RO4929097 treatment, the selected melanoma cell lines reveals downregulation of NOTCH downstream effector HES1. A decrease in the amount of melanospheres formed upon RO4929097 treatment in primary melanoma cell lines is detected.
in vivo: Oral injection of 3 to 60 mg/kg RO4929097 once daily or twice daily to nude mice bearing A549 NSCLC xenografts for either 7, 14, or 21 days of a 21-day schedule results in significant tumor growth inhibition compared with vehicle-treated animals. The tumor growth inhibition values ranges from 66% to 91%. When mice are treated with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule, treatment initially arouses regression of established A549 tumors. At the end of the 21-day cycle (day 47), tumor growth prevention is still 91% compared with vehicle control mice. Inhibition of tumor growth remains prolonged and sustained up to 34 days post-treatment (day 67). On day 67, these mice are retreated with the same dose of RO4929097 for a second cycle (7 days) until day 74. Importantly, the antitumor effects are sustained after dosing is completed [1]. RO4929097 leads to reduced expression of genes associated with angiogenesis in A549 xenograft model. In contrast, the RO4929097-resistant H460a xenograft displays little change in expression of these genes, underscoring the in vivo anti-angiogenesis mechanism of action of RO4929097.
For research and scientific purpose only, not for human use.
RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.
Product name: RO4929097 |Cat No. DC8215|Other names: RO4929097|Cas: 847925-91-1|Molecule Weight: 469.4|Molecule Formular: C22H20F5N3O3| Purity: >98%
RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.in vitro: RO4929097 decreases the amount of Aβ peptides secreted into the culture medium in HEK293 cells with EC50 of 14 nM. RO4929097 strongly inhibits Notch processing with EC50 of 5 nM in the Notch cell-based reporter assay. The potency of RO4929097 in cell-free and cellular assays is in the low nanomolar range with >100-fold selectivity observed with respect to 75 other proteins of various types including receptors, ion channels, and enzymes (CEREP panel). After 5 days of treatment, RO4929097 reduces the production of ICN in the human NSCLC A549 cells inducing a flattened and less transformed tumor cell phenotype in tissue culture . RO4929097 blocks Notch processing in human non-small cell lung carcinoma cells and decreases expression of the Notch transcriptional target gene Hes1. Treatment with RO4929097 reveals a two- to threefold decrease in the expression of direct Notch target genes, Hes1, Hey1, and Heyl in SUM149 and a 3.5- to eightfold decrease in expression in SUM190 cells. RO4929097 modestly inhibits the growth of SUM149 cells in a dose-dependent manner. At a concentration of 1 μM of RO4929097, growth inhibition is 20 % for SUM149 and 10 % for SUM190 cells, relative to vehicle-treated controls. RO4929097 decreases the production of inflammatory cytokines by T-cells. Furthermore, with RO4929097 treatment, there is a shift in favor of TH2 over TH1 cytokines. In addition, T-cell activation induced IL-6 production would be increased with RO4929097. Upon RO4929097 treatment, the selected melanoma cell lines reveals downregulation of NOTCH downstream effector HES1. A decrease in the amount of melanospheres formed upon RO4929097 treatment in primary melanoma cell lines is detected.
in vivo: Oral injection of 3 to 60 mg/kg RO4929097 once daily or twice daily to nude mice bearing A549 NSCLC xenografts for either 7, 14, or 21 days of a 21-day schedule results in significant tumor growth inhibition compared with vehicle-treated animals. The tumor growth inhibition values ranges from 66% to 91%. When mice are treated with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule, treatment initially arouses regression of established A549 tumors. At the end of the 21-day cycle (day 47), tumor growth prevention is still 91% compared with vehicle control mice. Inhibition of tumor growth remains prolonged and sustained up to 34 days post-treatment (day 67). On day 67, these mice are retreated with the same dose of RO4929097 for a second cycle (7 days) until day 74. Importantly, the antitumor effects are sustained after dosing is completed [1]. RO4929097 leads to reduced expression of genes associated with angiogenesis in A549 xenograft model. In contrast, the RO4929097-resistant H460a xenograft displays little change in expression of these genes, underscoring the in vivo anti-angiogenesis mechanism of action of RO4929097.
For research and scientific purpose only, not for human use.
NU6027|CDK Inhibitor|DC Chemicals
NU6027|CDK Inhibitor|DC Chemicals
NU 6027 inhibits both CDK1 and CDK2 with IC50 values of 2.9 and 2.2 µM, respectively.
Product name: NU6027 |Cat No. DC8214|Other names: NU6027 |Cas: 220036-08-8|Molecule Weight: 251.288|Molecule Formular: C11H17N5O2| Purity: >98%
NU 6027 inhibits both CDK1 and CDK2 with IC50 values of 2.9 and 2.2 µM, respectively. It has been shown to inhibit cellular ataxia telangiectasia mutated and Rad3-realted kinase activity (IC50 = 6.7 µM) and impair G2/M arrest in various human cancer cells, potentiating the cytotoxic effects of DNA-damaging, anticancer agents such as cisplatin.
For research and scientific purpose only, not for human use.
NU 6027 inhibits both CDK1 and CDK2 with IC50 values of 2.9 and 2.2 µM, respectively.
Product name: NU6027 |Cat No. DC8214|Other names: NU6027 |Cas: 220036-08-8|Molecule Weight: 251.288|Molecule Formular: C11H17N5O2| Purity: >98%
NU 6027 inhibits both CDK1 and CDK2 with IC50 values of 2.9 and 2.2 µM, respectively. It has been shown to inhibit cellular ataxia telangiectasia mutated and Rad3-realted kinase activity (IC50 = 6.7 µM) and impair G2/M arrest in various human cancer cells, potentiating the cytotoxic effects of DNA-damaging, anticancer agents such as cisplatin.
For research and scientific purpose only, not for human use.
ICA-121431|Nav1.7 channel inhibitor|DC Chemicals
ICA-121431|Nav1.7 channel inhibitor|DC Chemicals
ICA-121431 is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, but no inhibition on human, monkey and dog Nav1.7.
Product name: ICA-121431 |Cat No. DC8213|Other names: ICA-121431 |Cas: 313254-51-2|Molecule Weight: 449.54526|Molecule Formular: C23H19N3O3S2| Purity: >98%
ICA-121431 is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, but no inhibition on human, monkey and dog Nav1.7.ICA-121431 exhibited a spectrum of inhibitory activity for Nav human channel subtypes; equipotent inhibition of Nav1.3 and Nav1.1, less potent inhibition of Nav1.2, and much weaker inhibition of Nav1.7, Nav1.6, Nav1.4, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM). the unique subtype selective Nav channel inhibitors ICA-121431 and PF-04856264 interact with amino acid residues on an extracellular facing region of the homologous Domain 4 voltage sensor of Nav1.3 or Nav1.7, which is distinct from previously described interaction sites for TTX or local anesthetic-like Nav channel inhibitors.
For research and scientific purpose only, not for human use.
ICA-121431 is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, but no inhibition on human, monkey and dog Nav1.7.
Product name: ICA-121431 |Cat No. DC8213|Other names: ICA-121431 |Cas: 313254-51-2|Molecule Weight: 449.54526|Molecule Formular: C23H19N3O3S2| Purity: >98%
ICA-121431 is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, but no inhibition on human, monkey and dog Nav1.7.ICA-121431 exhibited a spectrum of inhibitory activity for Nav human channel subtypes; equipotent inhibition of Nav1.3 and Nav1.1, less potent inhibition of Nav1.2, and much weaker inhibition of Nav1.7, Nav1.6, Nav1.4, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM). the unique subtype selective Nav channel inhibitors ICA-121431 and PF-04856264 interact with amino acid residues on an extracellular facing region of the homologous Domain 4 voltage sensor of Nav1.3 or Nav1.7, which is distinct from previously described interaction sites for TTX or local anesthetic-like Nav channel inhibitors.
For research and scientific purpose only, not for human use.
OAC 1|iPSC reprogramming enhancer|DC Chemicals
OAC 1|iPSC reprogramming enhancer|DC Chemicals
OAC1 is a Octamer-binding transcription factor 4 (Oct4)-activating compound; enhances the iPSC reprogramming efficiency and accelerated the reprogramming process.
Product name: OAC1 |Cat No. DC8208|Other names: OAC1 |Cas: 300586-90-7|Molecule Weight: 237.26|Molecule Formular: C14H11N3O| Purity: >98%
OAC1 is a Octamer-binding transcription factor 4 (Oct4)-activating compound; enhances the iPSC reprogramming efficiency and accelerated the reprogramming process.in vitro: OAC1 enhances the formation of Oct4-GFP+ colonies and accelerates the dynamics of reprogramming. OAC1 enhanced reprogramming efficiency through a mechanism that is independent of endogenous Oct4 promoter demethylation. OAC1 enhanced reprogramming efficiency through a mechanism that is distinct from suppressing p53-p21 expression. Luciferase assay revealed that OAC1 had no effect on Topflash activity, although BIO activated the Topflash reporter potently. OAC1 functions through a mechanism that is independent of the Wnt signaling.
For research and scientific purpose only, not for human use.
OAC1 is a Octamer-binding transcription factor 4 (Oct4)-activating compound; enhances the iPSC reprogramming efficiency and accelerated the reprogramming process.
Product name: OAC1 |Cat No. DC8208|Other names: OAC1 |Cas: 300586-90-7|Molecule Weight: 237.26|Molecule Formular: C14H11N3O| Purity: >98%
OAC1 is a Octamer-binding transcription factor 4 (Oct4)-activating compound; enhances the iPSC reprogramming efficiency and accelerated the reprogramming process.in vitro: OAC1 enhances the formation of Oct4-GFP+ colonies and accelerates the dynamics of reprogramming. OAC1 enhanced reprogramming efficiency through a mechanism that is independent of endogenous Oct4 promoter demethylation. OAC1 enhanced reprogramming efficiency through a mechanism that is distinct from suppressing p53-p21 expression. Luciferase assay revealed that OAC1 had no effect on Topflash activity, although BIO activated the Topflash reporter potently. OAC1 functions through a mechanism that is independent of the Wnt signaling.
For research and scientific purpose only, not for human use.
Deltarasin|Kras inhibitor|DC Chemicals
Deltarasin|Kras inhibitor|DC Chemicals
Deltarasin is a novel and small molecule inhibitor which can inhibit the KRAS-PDEδ interaction(Kd= 41 nM. binding to PDEδ) and impairs oncogenic KRAS signalling.
Product name: Deltarasin |Cat No. DC8205|Other names: Deltarasin|Cas: 1440898-61-2|Molecule Weight: 603.75|Molecule Formular: C40H37N5O| Purity: >98%
Deltarasin is a novel and small molecule inhibitor which can inhibit the KRAS-PDEδ interaction(Kd= 41 nM. binding to PDEδ) and impairs oncogenic KRAS signalling.Interfering with binding of mammalian PDEδ to KRAS by means of small molecules provides a novel opportunity to suppress oncogenic RAS signalling by altering its localization to endomembranes. Biochemical screening and subsequent structure-based hit optimization yielded inhibitors of the KRAS-PDEδ interaction that selectively bind to the prenyl-binding pocket of PDEδ with nanomolar affinity, inhibit oncogenic RAS signalling and suppress in vitro and in vivo proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS.
For research and scientific purpose only, not for human use.
Deltarasin is a novel and small molecule inhibitor which can inhibit the KRAS-PDEδ interaction(Kd= 41 nM. binding to PDEδ) and impairs oncogenic KRAS signalling.
Product name: Deltarasin |Cat No. DC8205|Other names: Deltarasin|Cas: 1440898-61-2|Molecule Weight: 603.75|Molecule Formular: C40H37N5O| Purity: >98%
Deltarasin is a novel and small molecule inhibitor which can inhibit the KRAS-PDEδ interaction(Kd= 41 nM. binding to PDEδ) and impairs oncogenic KRAS signalling.Interfering with binding of mammalian PDEδ to KRAS by means of small molecules provides a novel opportunity to suppress oncogenic RAS signalling by altering its localization to endomembranes. Biochemical screening and subsequent structure-based hit optimization yielded inhibitors of the KRAS-PDEδ interaction that selectively bind to the prenyl-binding pocket of PDEδ with nanomolar affinity, inhibit oncogenic RAS signalling and suppress in vitro and in vivo proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS.
For research and scientific purpose only, not for human use.
b-AP15(NSC687852)|deubiquitinating enzymes inhibitor|DC Chemicals
b-AP15(NSC687852)|deubiquitinating enzymes inhibitor|DC Chemicals
b-AP15(NSC687852) is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14 of the 26S proteasome. It blocks the deubiquitinating activity of the 26S proteasome.
Product name: b-AP15(NSC687852) |Cat No. DC8203|Other names: NSC-687852|Cas: 1009817-63-3|Molecule Weight: 419.39|Molecule Formular: C22H17N3O6| Purity: >98%
b-AP15(NSC687852) is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14 of the 26S proteasome. It blocks the deubiquitinating activity of the 26S proteasome.in vitro: b-AP15 abrogates the deubiquitinating activity of the 19S regulatory particle.b-AP15 inhibited the activity of two 19S regulatory-particle-associated deubiquitinases, ubiquitin C-terminal hydrolase 5 (UCHL5) and ubiquitin-specific peptidase 14 (USP14), resulting in accumulation of polyubiquitin. b-AP15 induced tumor cell apoptosis that was insensitive to TP53 status and overexpression of the apoptosis inhibitor BCL2. b-AP15 triggers time- and dose-dependent apoptosis of the human multiple myeloma (MM) cell lines RPMI8226 and U266, as determined by phosphatidylserine exposure. Apoptosis was dependent on caspase activation and was partially dependent on cathepsin D. Furthermore, b-AP15 triggered processing of pro-caspase-3 and cleavage of poly (ADP-ribose) polymerase in MM cells. b-AP15 also induced caspase-independent apoptosis in primary human natural killer cells. in addition to inhibition of deubiquitinases, b-AP15 inhibits the selenoprotein thioredoxin reductase (TrxR）.
in vivo: Treatment with b-AP15 inhibited tumor progression in four different in vivo solid tumor models and inhibited organ infiltration in an acute myeloid leukemia model [1]. b-AP15 is well tolerated, inhibits tumor growth, and prolongs survival. Combining b-AP15 with suberoylanilide hydroxamic acid, lenalidomide, or dexamethasone induces synergistic anti-MM activity in distinct human MM xenograft models.
For research and scientific purpose only, not for human use.
b-AP15(NSC687852) is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14 of the 26S proteasome. It blocks the deubiquitinating activity of the 26S proteasome.
Product name: b-AP15(NSC687852) |Cat No. DC8203|Other names: NSC-687852|Cas: 1009817-63-3|Molecule Weight: 419.39|Molecule Formular: C22H17N3O6| Purity: >98%
b-AP15(NSC687852) is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14 of the 26S proteasome. It blocks the deubiquitinating activity of the 26S proteasome.in vitro: b-AP15 abrogates the deubiquitinating activity of the 19S regulatory particle.b-AP15 inhibited the activity of two 19S regulatory-particle-associated deubiquitinases, ubiquitin C-terminal hydrolase 5 (UCHL5) and ubiquitin-specific peptidase 14 (USP14), resulting in accumulation of polyubiquitin. b-AP15 induced tumor cell apoptosis that was insensitive to TP53 status and overexpression of the apoptosis inhibitor BCL2. b-AP15 triggers time- and dose-dependent apoptosis of the human multiple myeloma (MM) cell lines RPMI8226 and U266, as determined by phosphatidylserine exposure. Apoptosis was dependent on caspase activation and was partially dependent on cathepsin D. Furthermore, b-AP15 triggered processing of pro-caspase-3 and cleavage of poly (ADP-ribose) polymerase in MM cells. b-AP15 also induced caspase-independent apoptosis in primary human natural killer cells. in addition to inhibition of deubiquitinases, b-AP15 inhibits the selenoprotein thioredoxin reductase (TrxR）.
in vivo: Treatment with b-AP15 inhibited tumor progression in four different in vivo solid tumor models and inhibited organ infiltration in an acute myeloid leukemia model [1]. b-AP15 is well tolerated, inhibits tumor growth, and prolongs survival. Combining b-AP15 with suberoylanilide hydroxamic acid, lenalidomide, or dexamethasone induces synergistic anti-MM activity in distinct human MM xenograft models.
For research and scientific purpose only, not for human use.
Firategrast(SB-683699)|integrin antagonist|DC Chemicals
Firategrast(SB-683699)|integrin antagonist|DC Chemicals
Firategrast is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS).
Product name: Firategrast(SB-683699) |Cat No. DC8200|Other names: Firategrast(SB-683699)|Cas: 402567-16-2|Molecule Weight: 499.5|Molecule Formular: C27H27F2NO6| Purity: >98%
Firategrast is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS). in vivo: Median (n, range) CSF lymphocyte counts (cells/?l) at weeks 0, 24, 28 and 36 were: 5.3 (44, 0.3-70.2), 3.3 (31, 0.0-99.0), 3.0 (32, 0.0-58.2) and 3.5 (29, 0.0-274.8). CD4+, CD8+ T- and CD19+ B-lymphocyte counts followed a similar pattern. Minimal changes were observed for CD3-CD16+CD56+ natural killer cells. Median CD4 : CD8 ratios were: 2.9 (41, 1.1-10.9), 2.2 (29, 0.6-5.9), 3.8 (28, 1.6-9.0) and 3.8 (21, 2.1-9.4). Blood lymphocyte counts were elevated at weeks 4 and 24, consistent with the mechanism of firategrast, and returned to baseline when firategrast was discontinued.
Toxicity: Firategrast was generally well tolerated at all doses. The frequency of all adverse events was similar across all treatment groups except for an increased rate of urinary tract infections in the high-dose firategrast group. No cases of progressive multifocal leukoencephalopathy or evidence of reactivation of JC virus were identified.
For research and scientific purpose only, not for human use.
Firategrast is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS).
Product name: Firategrast(SB-683699) |Cat No. DC8200|Other names: Firategrast(SB-683699)|Cas: 402567-16-2|Molecule Weight: 499.5|Molecule Formular: C27H27F2NO6| Purity: >98%
Firategrast is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS). in vivo: Median (n, range) CSF lymphocyte counts (cells/?l) at weeks 0, 24, 28 and 36 were: 5.3 (44, 0.3-70.2), 3.3 (31, 0.0-99.0), 3.0 (32, 0.0-58.2) and 3.5 (29, 0.0-274.8). CD4+, CD8+ T- and CD19+ B-lymphocyte counts followed a similar pattern. Minimal changes were observed for CD3-CD16+CD56+ natural killer cells. Median CD4 : CD8 ratios were: 2.9 (41, 1.1-10.9), 2.2 (29, 0.6-5.9), 3.8 (28, 1.6-9.0) and 3.8 (21, 2.1-9.4). Blood lymphocyte counts were elevated at weeks 4 and 24, consistent with the mechanism of firategrast, and returned to baseline when firategrast was discontinued.
Toxicity: Firategrast was generally well tolerated at all doses. The frequency of all adverse events was similar across all treatment groups except for an increased rate of urinary tract infections in the high-dose firategrast group. No cases of progressive multifocal leukoencephalopathy or evidence of reactivation of JC virus were identified.
For research and scientific purpose only, not for human use.
Tyrosine kinase inhibitor
Tyrosine kinase inhibitor|DC Chemicals
A Tyrosine kinase inhibitor.
Product name: Tyrosine kinase inhibitor |Cat No. DC8197|Other names: Tyrosine kinase inhibitor |Cas: 1021950-26-4|Molecule Weight: 586.6134432|Molecule Formular: C31H31FN6O5| Purity: >98%
A Tyrosine kinase inhibitor.
For research and scientific purpose only, not for human use.
A Tyrosine kinase inhibitor.
Product name: Tyrosine kinase inhibitor |Cat No. DC8197|Other names: Tyrosine kinase inhibitor |Cas: 1021950-26-4|Molecule Weight: 586.6134432|Molecule Formular: C31H31FN6O5| Purity: >98%
A Tyrosine kinase inhibitor.
For research and scientific purpose only, not for human use.
FG2216|HIF-prolyl hydroxylase inhibitor|DC Chemicals
FG2216|HIF-prolyl hydroxylase inhibitor|DC Chemicals
FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.
Product name: FG2216 |Cat No. DC8195|Other names: FG2216|Cas: 223387-75-5|Molecule Weight: 280.66|Molecule Formular: C12H9ClN2O4| Purity: >98%
FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.
FG-2216 was orally bioavailable and induced significant and reversible Epo induction in vivo (82- to 309-fold at 60 mg/kg). Chronic oral dosing in male rhesus macaques was well tolerated, significantly increased erythropoiesis, and prevented anemia induced by weekly phlebotomy. Furthermore, modest increases in HbF-containing red cells and reticulocytes were demonstrated by flow cytometry, though significant increases in HbF were not demonstrated by high-pressure liquid chromatography (HPLC).
For research and scientific purpose only, not for human use.
FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.
Product name: FG2216 |Cat No. DC8195|Other names: FG2216|Cas: 223387-75-5|Molecule Weight: 280.66|Molecule Formular: C12H9ClN2O4| Purity: >98%
FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.
FG-2216 was orally bioavailable and induced significant and reversible Epo induction in vivo (82- to 309-fold at 60 mg/kg). Chronic oral dosing in male rhesus macaques was well tolerated, significantly increased erythropoiesis, and prevented anemia induced by weekly phlebotomy. Furthermore, modest increases in HbF-containing red cells and reticulocytes were demonstrated by flow cytometry, though significant increases in HbF were not demonstrated by high-pressure liquid chromatography (HPLC).
For research and scientific purpose only, not for human use.
PP3，Negative control for PP2|DC Chemicals
PP3，Negative control for PP2|DC Chemicals
Negative control for the Src kinase inhibitor PP2.
Product name: PP3 |Cat No. DC8194|Other names: PP3|Cas: 5334-30-5|Molecule Weight: 211.23|Molecule Formular: C11H9N5| Purity: >98%
Negative control for the Src kinase inhibitor PP2. Inhibits EGFR kinase (IC50 = 2.7 μM).
For research and scientific purpose only, not for human use.
Negative control for the Src kinase inhibitor PP2.
Product name: PP3 |Cat No. DC8194|Other names: PP3|Cas: 5334-30-5|Molecule Weight: 211.23|Molecule Formular: C11H9N5| Purity: >98%
Negative control for the Src kinase inhibitor PP2. Inhibits EGFR kinase (IC50 = 2.7 μM).
For research and scientific purpose only, not for human use.
KPT-9274|PAMs|PAK4 Allosteric Modulator|DC Chemicals
KPT-9274|PAMs|PAK4 Allosteric Modulator|DC Chemicals
KPT-9274 is a PAK4 Allosteric Modulator(PAM).
Product name: KPT-9274 |Cat No. DC8192|Other names: KPT 9274，KPT9274，KPT 9274|Cas: N/A|Molecule Weight: 610.22|Molecule Formular: C35H29F3N4O3| Purity: >98%
KPT-9274 is a PAK4 Allosteric Modulator(PAM).
For research and scientific purpose only, not for human use.
KPT-9274 is a PAK4 Allosteric Modulator(PAM).
Product name: KPT-9274 |Cat No. DC8192|Other names: KPT 9274，KPT9274，KPT 9274|Cas: N/A|Molecule Weight: 610.22|Molecule Formular: C35H29F3N4O3| Purity: >98%
KPT-9274 is a PAK4 Allosteric Modulator(PAM).
For research and scientific purpose only, not for human use.
Sparsentan(PS433540)|Supplied by DC Chemicals
Sparsentan(PS433540)|Supplied by DC Chemicals
acting as both an Endothelin Receptor Antagonist (ERA) and Angiotensin Receptor Blocker (ARB).
Product name: Sparsentan(PS433540) |Cat No. DC8191|Other names: Sparsentan, PS433540|Cas: 254740-64-2|Molecule Weight: 592.27|Molecule Formular: C32H40N4O5S| Purity: >98%
For research and scientific purpose only, not for human use.
acting as both an Endothelin Receptor Antagonist (ERA) and Angiotensin Receptor Blocker (ARB).
Product name: Sparsentan(PS433540) |Cat No. DC8191|Other names: Sparsentan, PS433540|Cas: 254740-64-2|Molecule Weight: 592.27|Molecule Formular: C32H40N4O5S| Purity: >98%
For research and scientific purpose only, not for human use.
Ravidasvir(PPI-668)|Supplied by DC Chemicals
Ravidasvir(PPI-668)|Supplied by DC Chemicals
NS5A Inhibitor
Product name: Ravidasvir(PPI-668) |Cat No. DC8190|Other names: Ravidasvir, PPI-668|Cas: 1242087-93-9|Molecule Weight: 762.38|Molecule Formular: C42H50N8O6| Purity: >98%
For research and scientific purpose only, not for human use.
NS5A Inhibitor
Product name: Ravidasvir(PPI-668) |Cat No. DC8190|Other names: Ravidasvir, PPI-668|Cas: 1242087-93-9|Molecule Weight: 762.38|Molecule Formular: C42H50N8O6| Purity: >98%
For research and scientific purpose only, not for human use.
Etelcalcetide Hydrochloride(AMG 416)|Supplied by DC Chemicals
Etelcalcetide Hydrochloride(AMG 416)|Supplied by DC Chemicals
Activates calcium sensing receptor on parathyroid glands reducing PTH synthesis and secretion
Product name: Etelcalcetide Hydrochloride(AMG 416) |Cat No. DC8189|Other names: Etelcalcetide Hydrochloride, AMG 416|Cas: 1334237-71-6|Molecule Weight: 1097.53|Molecule Formular: C38H76ClN23O9S2| Purity: >98%
For research and scientific purpose only, not for human use.
Activates calcium sensing receptor on parathyroid glands reducing PTH synthesis and secretion
Product name: Etelcalcetide Hydrochloride(AMG 416) |Cat No. DC8189|Other names: Etelcalcetide Hydrochloride, AMG 416|Cas: 1334237-71-6|Molecule Weight: 1097.53|Molecule Formular: C38H76ClN23O9S2| Purity: >98%
For research and scientific purpose only, not for human use.
Daprodustat(GSK1278863)|Supplied by DC Chemicals
Daprodustat(GSK1278863)|Supplied by DC Chemicals
HIF-prolyl hydroxylase inhibitor
Product name: Daprodustat(GSK1278863) |Cat No. DC8188|Other names: Daprodustat, GSK1278863|Cas: 960539-70-2|Molecule Weight: 393.18|Molecule Formular: C19H27N3O6| Purity: >98%
For research and scientific purpose only, not for human use.
HIF-prolyl hydroxylase inhibitor
Product name: Daprodustat(GSK1278863) |Cat No. DC8188|Other names: Daprodustat, GSK1278863|Cas: 960539-70-2|Molecule Weight: 393.18|Molecule Formular: C19H27N3O6| Purity: >98%
For research and scientific purpose only, not for human use.
Ciraparantag(PER977)|Supplied by DC Chemicals
Ciraparantag(PER977)|Supplied by DC Chemicals
an intravenously administered anticoagulant Reversal Agent
Product name: Ciraparantag(PER977) |Cat No. DC8187|Other names: Ciraparantag, PER977|Cas: 1438492-26-2|Molecule Weight: 512.4|Molecule Formular: C22H48N12O2| Purity: >98%
For research and scientific purpose only, not for human use.
an intravenously administered anticoagulant Reversal Agent
Product name: Ciraparantag(PER977) |Cat No. DC8187|Other names: Ciraparantag, PER977|Cas: 1438492-26-2|Molecule Weight: 512.4|Molecule Formular: C22H48N12O2| Purity: >98%
For research and scientific purpose only, not for human use.
Bexagliflozin(THR1442)|Supplied by DC Chemicals
Bexagliflozin(THR1442)|Supplied by DC Chemicals
SGLT2 inhibitor
Product name: Bexagliflozin(THR1442) |Cat No. DC8186|Other names: Bexagliflozin, THR1442|Cas: 1118567-05-7|Molecule Weight: 464.16|Molecule Formular: C24H29ClO7| Purity: >98%
For research and scientific purpose only, not for human use.
SGLT2 inhibitor
Product name: Bexagliflozin(THR1442) |Cat No. DC8186|Other names: Bexagliflozin, THR1442|Cas: 1118567-05-7|Molecule Weight: 464.16|Molecule Formular: C24H29ClO7| Purity: >98%
For research and scientific purpose only, not for human use.
Verosudil(AR-12286)|Supplied by DC Chemicals
Verosudil(AR-12286)|Supplied by DC Chemicals
Rho-kinase (ROCK) inhibitor
Product name: Verosudil(AR-12286) |Cat No. DC8185|Other names: Verosudil, AR-12286|Cas: 1414854-42-4|Molecule Weight: 327.1|Molecule Formular: C17H17N3O2S| Purity: >98%
For research and scientific purpose only, not for human use.
Rho-kinase (ROCK) inhibitor
Product name: Verosudil(AR-12286) |Cat No. DC8185|Other names: Verosudil, AR-12286|Cas: 1414854-42-4|Molecule Weight: 327.1|Molecule Formular: C17H17N3O2S| Purity: >98%
For research and scientific purpose only, not for human use.
Pilaralisib(XL-147; SAR245408)|Supplied by DC Chemicals
Pilaralisib(XL-147; SAR245408)|Supplied by DC Chemicals
Pilaralisib (SAR245408; XL147) is selective oral pan-PI3K inhibitor.
Product name: Pilaralisib(XL-147; SAR245408) |Cat No. DC8184|Other names: Pilaralisib, XL-147; SAR245408|Cas: 934526-89-3|Molecule Weight: 540.13|Molecule Formular: C25H25ClN6O4S| Purity: >98%
Pilaralisib, also known as XL147, is a Class 1 PI3K kinase family inhibitor, and is an orally bioavailable small molecule, targeting the class I phosphatidylinositol 3 kinase (PI3K) family of lipid kinases, with potential antineoplastic activity. Class 1 PI3K kinase family inhibitor XL147 reversibly binds to class 1 PI3Ks in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K signaling pathway; this may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents including genotoxic agents and receptor tyrosine kinase inhibitors.
For research and scientific purpose only, not for human use.
Pilaralisib (SAR245408; XL147) is selective oral pan-PI3K inhibitor.
Product name: Pilaralisib(XL-147; SAR245408) |Cat No. DC8184|Other names: Pilaralisib, XL-147; SAR245408|Cas: 934526-89-3|Molecule Weight: 540.13|Molecule Formular: C25H25ClN6O4S| Purity: >98%
Pilaralisib, also known as XL147, is a Class 1 PI3K kinase family inhibitor, and is an orally bioavailable small molecule, targeting the class I phosphatidylinositol 3 kinase (PI3K) family of lipid kinases, with potential antineoplastic activity. Class 1 PI3K kinase family inhibitor XL147 reversibly binds to class 1 PI3Ks in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K signaling pathway; this may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents including genotoxic agents and receptor tyrosine kinase inhibitors.
For research and scientific purpose only, not for human use.
Paritaprevir(Veruprevir ABT-450)|Supplied by DC Chemicals
Paritaprevir(Veruprevir ABT-450)|Supplied by DC Chemicals
NS3/4A protease inhibitor
Product name: Paritaprevir(Veruprevir ABT-450) |Cat No. DC8183|Other names: Paritaprevir, Veruprevir ABT-450|Cas: 1216941-48-8|Molecule Weight: 765.29|Molecule Formular: C40H43N7O7S| Purity: >98%
For research and scientific purpose only, not for human use.
NS3/4A protease inhibitor
Product name: Paritaprevir(Veruprevir ABT-450) |Cat No. DC8183|Other names: Paritaprevir, Veruprevir ABT-450|Cas: 1216941-48-8|Molecule Weight: 765.29|Molecule Formular: C40H43N7O7S| Purity: >98%
For research and scientific purpose only, not for human use.
Bempedoic Acid(ETC-1002;ESP-55016)|Supplied by DC Chemicals
Bempedoic Acid(ETC-1002;ESP-55016)|Supplied by DC Chemicals
ATP citrate lyase inhibitor;AMP-activated protein kinase (AMPK) activator
Product name: Bempedoic Acid(ETC-1002;ESP-55016) |Cat No. DC8182|Other names: Bempedoic Acid, ETC-1002;ESP-55016|Cas: 738606-46-7|Molecule Weight: 344.25|Molecule Formular: C19H36O5| Purity: >98%
For research and scientific purpose only, not for human use.
ATP citrate lyase inhibitor;AMP-activated protein kinase (AMPK) activator
Product name: Bempedoic Acid(ETC-1002;ESP-55016) |Cat No. DC8182|Other names: Bempedoic Acid, ETC-1002;ESP-55016|Cas: 738606-46-7|Molecule Weight: 344.25|Molecule Formular: C19H36O5| Purity: >98%
For research and scientific purpose only, not for human use.
Filanesib(ARRY-520)|Supplied by DC Chemicals
Filanesib(ARRY-520)|Supplied by DC Chemicals
Kinesin spindle protein Inhibitor
Product name: Filanesib(ARRY-520) |Cat No. DC8181|Other names: Filanesib, ARRY-520|Cas: 885060-09-3|Molecule Weight: 420.14|Molecule Formular: C20H22F2N4O2S| Purity: >98%
For research and scientific purpose only, not for human use.
Kinesin spindle protein Inhibitor
Product name: Filanesib(ARRY-520) |Cat No. DC8181|Other names: Filanesib, ARRY-520|Cas: 885060-09-3|Molecule Weight: 420.14|Molecule Formular: C20H22F2N4O2S| Purity: >98%
For research and scientific purpose only, not for human use.
2015年6月23日星期二
Cabotegravir(GSK1265744A,GSK-744)|Supplied by DC Chemicals
Cabotegravir(GSK1265744A,GSK-744)|Supplied by DC Chemicals
integrase inhibitor
Product name: Cabotegravir(GSK1265744A,GSK-744) |Cat No. DC8180|Other names: Cabotegravir, GSK1265744A,GSK-744|Cas: 1051375-10-0|Molecule Weight: 405.11|Molecule Formular: C19H17F2N3O5| Purity: >98%
For research and scientific purpose only, not for human use.
integrase inhibitor
Product name: Cabotegravir(GSK1265744A,GSK-744) |Cat No. DC8180|Other names: Cabotegravir, GSK1265744A,GSK-744|Cas: 1051375-10-0|Molecule Weight: 405.11|Molecule Formular: C19H17F2N3O5| Purity: >98%
For research and scientific purpose only, not for human use.
Briciclib(ON 013105,ON 014185)|Supplied by DC Chemicals
Briciclib(ON 013105,ON 014185)|Supplied by DC Chemicals
Product name: Briciclib(ON 013105,ON 014185) |Cat No. DC8179|Other names: Briciclib, ON 013105,ON 014185|Cas: 865783-99-9|Molecule Weight: 474.07|Molecule Formular: C19H23O10PS| Purity: >98%
For research and scientific purpose only, not for human use.
Product name: Briciclib(ON 013105,ON 014185) |Cat No. DC8179|Other names: Briciclib, ON 013105,ON 014185|Cas: 865783-99-9|Molecule Weight: 474.07|Molecule Formular: C19H23O10PS| Purity: >98%
For research and scientific purpose only, not for human use.
Beclabuvir(BMS-791325)|Supplied by DC Chemicals
Beclabuvir(BMS-791325)|Supplied by DC Chemicals
non-nucleoside inhibitor of the NS5B
Product name: Beclabuvir(BMS-791325) |Cat No. DC8178|Other names: Beclabuvir, BMS-791325|Cas: 958002-33-0|Molecule Weight: 659.31|Molecule Formular: C36H45N5O5S| Purity: >98%
For research and scientific purpose only, not for human use.
non-nucleoside inhibitor of the NS5B
Product name: Beclabuvir(BMS-791325) |Cat No. DC8178|Other names: Beclabuvir, BMS-791325|Cas: 958002-33-0|Molecule Weight: 659.31|Molecule Formular: C36H45N5O5S| Purity: >98%
For research and scientific purpose only, not for human use.
Enclomiphene citrate|Supplied by DC Chemicals
Enclomiphene citrate|Supplied by DC Chemicals
Product name: Enclomiphene citrate |Cat No. DC8177|Other names: Enclomiphene citrate|Cas: 7599-79-3|Molecule Weight: 597.21|Molecule Formular: C32H36ClNO8| Purity: >98%
For research and scientific purpose only, not for human use.
Product name: Enclomiphene citrate |Cat No. DC8177|Other names: Enclomiphene citrate|Cas: 7599-79-3|Molecule Weight: 597.21|Molecule Formular: C32H36ClNO8| Purity: >98%
For research and scientific purpose only, not for human use.
Tradipitant(VLY-686)|Supplied by DC Chemicals
Tradipitant(VLY-686)|Supplied by DC Chemicals
Product name: Tradipitant(VLY-686) |Cat No. DC8176|Other names: Tradipitant, VLY-686|Cas: 622370-35-8|Molecule Weight: 587.09|Molecule Formular: C28H16ClF6N5O| Purity: >98%
For research and scientific purpose only, not for human use.
Product name: Tradipitant(VLY-686) |Cat No. DC8176|Other names: Tradipitant, VLY-686|Cas: 622370-35-8|Molecule Weight: 587.09|Molecule Formular: C28H16ClF6N5O| Purity: >98%
For research and scientific purpose only, not for human use.
Rapastinel(GLYX-13)|NMDA receptor partial agonist|DC Chemicals
Rapastinel(GLYX-13)|NMDA receptor partial agonist|DC Chemicals
Rapastinel(GLYX-13) is a NMDA receptor partial agonist that acts at the glycine site.
Product name: Rapastinel(GLYX-13) |Cat No. DC8175|Other names: Rapastinel, GLYX-13|Cas: 117928-94-6|Molecule Weight: 413.22|Molecule Formular: C18H31N5O6| Purity: >98%
NMDA receptor partial agonist that acts at the glycine site. Simultaneously acts as a promoter of the induction of long-term potentiation (LTP) and as a suppressor of long-term depression (LTD). Exhibits nootropic, neuroprotective and antinociceptive activity, and enhances learning, memory and cognition in vivo. Brain penetrant.
For research and scientific purpose only, not for human use.
Rapastinel(GLYX-13) is a NMDA receptor partial agonist that acts at the glycine site.
Product name: Rapastinel(GLYX-13) |Cat No. DC8175|Other names: Rapastinel, GLYX-13|Cas: 117928-94-6|Molecule Weight: 413.22|Molecule Formular: C18H31N5O6| Purity: >98%
NMDA receptor partial agonist that acts at the glycine site. Simultaneously acts as a promoter of the induction of long-term potentiation (LTP) and as a suppressor of long-term depression (LTD). Exhibits nootropic, neuroprotective and antinociceptive activity, and enhances learning, memory and cognition in vivo. Brain penetrant.
For research and scientific purpose only, not for human use.
Pexmetinib(ARRY-614)|Supplied by DC Chemicals
Pexmetinib(ARRY-614)|Supplied by DC Chemicals
Product name: Pexmetinib(ARRY-614) |Cat No. DC8174|Other names: Pexmetinib, ARRY-614|Cas: 945614-12-0|Molecule Weight: 556.25|Molecule Formular: C31H33FN6O3| Purity: >98%
For research and scientific purpose only, not for human use.
Product name: Pexmetinib(ARRY-614) |Cat No. DC8174|Other names: Pexmetinib, ARRY-614|Cas: 945614-12-0|Molecule Weight: 556.25|Molecule Formular: C31H33FN6O3| Purity: >98%
For research and scientific purpose only, not for human use.
Lemborexant(E2006)|Supplied by DC Chemicals
Lemborexant(E2006)|Supplied by DC Chemicals
Product name: Lemborexant(E2006) |Cat No. DC8173|Other names: Lemborexant, E2006|Cas: 1369764-02-2|Molecule Weight: 410.42|Molecule Formular: C22H20F2N4O2| Purity: >98%
For research and scientific purpose only, not for human use.
Product name: Lemborexant(E2006) |Cat No. DC8173|Other names: Lemborexant, E2006|Cas: 1369764-02-2|Molecule Weight: 410.42|Molecule Formular: C22H20F2N4O2| Purity: >98%
For research and scientific purpose only, not for human use.
Lefamulin(BC-3781)|Supplied by DC Chemicals
Lefamulin(BC-3781)|Supplied by DC Chemicals
Product name: Lefamulin(BC-3781) |Cat No. DC8172|Other names: Lefamulin, BC-3781|Cas: 1061337-51-6|Molecule Weight: 507.3|Molecule Formular: C28H45NO5S| Purity: >98%
For research and scientific purpose only, not for human use.
Product name: Lefamulin(BC-3781) |Cat No. DC8172|Other names: Lefamulin, BC-3781|Cas: 1061337-51-6|Molecule Weight: 507.3|Molecule Formular: C28H45NO5S| Purity: >98%
For research and scientific purpose only, not for human use.
decernotinib (VX-509,adelatinib)|Supplied by DC Chemicals
decernotinib (VX-509,adelatinib)|Supplied by DC Chemicals
Product name: decernotinib (VX-509,adelatinib) |Cat No. DC8171|Other names: decernotinib , VX-509,adelatinib|Cas: 944842-54-0|Molecule Weight: 392.15|Molecule Formular: C18H19F3N6O| Purity: >98%
For research and scientific purpose only, not for human use.
Product name: decernotinib (VX-509,adelatinib) |Cat No. DC8171|Other names: decernotinib , VX-509,adelatinib|Cas: 944842-54-0|Molecule Weight: 392.15|Molecule Formular: C18H19F3N6O| Purity: >98%
For research and scientific purpose only, not for human use.
Solcitinib（GSK2586184,GLPG0778）|Supplied by DC Chemicals
Solcitinib（GSK2586184,GLPG0778）|Supplied by DC Chemicals
Janus kinase 1 (JAK1) inhibitor
Product name: Solcitinib（GSK2586184,GLPG0778） |Cat No. DC8169|Other names: Solcitinib, GSK2586184,GLPG0778|Cas: 1206163-45-2|Molecule Weight: 389.18|Molecule Formular: C22H23N5O2| Purity: >98%
For research and scientific purpose only, not for human use.
Janus kinase 1 (JAK1) inhibitor
Product name: Solcitinib（GSK2586184,GLPG0778） |Cat No. DC8169|Other names: Solcitinib, GSK2586184,GLPG0778|Cas: 1206163-45-2|Molecule Weight: 389.18|Molecule Formular: C22H23N5O2| Purity: >98%
For research and scientific purpose only, not for human use.
Peficitinb（ASP015K,JNJ-54781532）|Supplied by DC Chemicals
Peficitinb（ASP015K,JNJ-54781532）|Supplied by DC Chemicals
JAK inhibitor
Product name: Peficitinb（ASP015K,JNJ-54781532） |Cat No. DC8168|Other names: Peficitinb, ASP015K,JNJ-54781532|Cas: 944118-01-8|Molecule Weight: 326.17|Molecule Formular: C18H22N4O2| Purity: >98%
For research and scientific purpose only, not for human use.
JAK inhibitor
Product name: Peficitinb（ASP015K,JNJ-54781532） |Cat No. DC8168|Other names: Peficitinb, ASP015K,JNJ-54781532|Cas: 944118-01-8|Molecule Weight: 326.17|Molecule Formular: C18H22N4O2| Purity: >98%
For research and scientific purpose only, not for human use.
Onalespib（AT13387,ATI13387X）|Supplied by DC Chemicals
Onalespib（AT13387,ATI13387X）|Supplied by DC Chemicals
Hsp90 inhibitor
Product name: Onalespib（AT13387,ATI13387X） |Cat No. DC8167|Other names: Onalespib, AT13387,ATI13387X|Cas: 912999-49-6|Molecule Weight: 409.23|Molecule Formular: C24H31N3O3| Purity: >98%
For research and scientific purpose only, not for human use.
Hsp90 inhibitor
Product name: Onalespib（AT13387,ATI13387X） |Cat No. DC8167|Other names: Onalespib, AT13387,ATI13387X|Cas: 912999-49-6|Molecule Weight: 409.23|Molecule Formular: C24H31N3O3| Purity: >98%
For research and scientific purpose only, not for human use.
Molidustat(BAY 85-3934)|Supplied by DC Chemicals
Molidustat(BAY 85-3934)|Supplied by DC Chemicals
Hypoxia-inducible factor prolyl hydroxylase inhibitor
Product name: Molidustat(BAY 85-3934) |Cat No. DC8166|Other names: Molidustat, BAY 85-3934|Cas: 1154028-82-6|Molecule Weight: 314.12|Molecule Formular: C13H14N8O2| Purity: >98%
Molidustat, also known as BAY 85-3934, is a novel inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH) which stimulates erythropoietin (EPO) production and the formation of red blood cells. Phase I data have shown that inhibition of HIF-PH by Molidustat results in an increase in endogenous production of EPO. Molidustat is currently clinical trials at Bayer for the treatment of patients suffering from renal anemia due to chronic kidney disease.
For research and scientific purpose only, not for human use.
Hypoxia-inducible factor prolyl hydroxylase inhibitor
Product name: Molidustat(BAY 85-3934) |Cat No. DC8166|Other names: Molidustat, BAY 85-3934|Cas: 1154028-82-6|Molecule Weight: 314.12|Molecule Formular: C13H14N8O2| Purity: >98%
Molidustat, also known as BAY 85-3934, is a novel inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH) which stimulates erythropoietin (EPO) production and the formation of red blood cells. Phase I data have shown that inhibition of HIF-PH by Molidustat results in an increase in endogenous production of EPO. Molidustat is currently clinical trials at Bayer for the treatment of patients suffering from renal anemia due to chronic kidney disease.
For research and scientific purpose only, not for human use.
Gilteritinib(ASP2215)|Supplied by DC Chemicals
Gilteritinib(ASP2215)|Supplied by DC Chemicals
FLT3/AXL inhibitor
Product name: Gilteritinib(ASP2215) |Cat No. DC8164|Other names: Gilteritinib, ASP2215|Cas: 1254053-43-4|Molecule Weight: 552.35|Molecule Formular: C29H44N8O3| Purity: >98%
For research and scientific purpose only, not for human use.
FLT3/AXL inhibitor
Product name: Gilteritinib(ASP2215) |Cat No. DC8164|Other names: Gilteritinib, ASP2215|Cas: 1254053-43-4|Molecule Weight: 552.35|Molecule Formular: C29H44N8O3| Purity: >98%
For research and scientific purpose only, not for human use.
Fostemsavir(BMS-663068)|Supplied by DC Chemicals
Fostemsavir(BMS-663068)|Supplied by DC Chemicals
HIV-1 attachment inhibitor,a prodrug of the small-molecule inhibitor BMS-626529
Product name: Fostemsavir(BMS-663068) |Cat No. DC8163|Other names: Fostemsavir, BMS-663068|Cas: 864953-29-7|Molecule Weight: 583.15|Molecule Formular: C25H26N7O8P| Purity: >98%
Fostemsavir (also known as BMS-663068) is an investigational drug that is being studied for the treatment of HIV infection. Fostemsavir belongs to a class (group) of HIV drugs called entry and fusion inhibitors.2 Entry and fusion inhibitors block HIV from getting into and infecting certain cells of the immune system. This prevents HIV from multiplying and can reduce the amount of HIV in the body.By attaching to the gp120 protein on the outer surface of HIV, fostemsavir blocks HIV from getting into and infecting the immune cells.
Fostemsavir is a prodrug, which means that it is an inactive drug. Once taken, a prodrug does not work until the body converts it into an active form. In the body, fostemsavir is converted to temsavir (also known as BMS-626529).
For research and scientific purpose only, not for human use.
HIV-1 attachment inhibitor,a prodrug of the small-molecule inhibitor BMS-626529
Product name: Fostemsavir(BMS-663068) |Cat No. DC8163|Other names: Fostemsavir, BMS-663068|Cas: 864953-29-7|Molecule Weight: 583.15|Molecule Formular: C25H26N7O8P| Purity: >98%
Fostemsavir (also known as BMS-663068) is an investigational drug that is being studied for the treatment of HIV infection. Fostemsavir belongs to a class (group) of HIV drugs called entry and fusion inhibitors.2 Entry and fusion inhibitors block HIV from getting into and infecting certain cells of the immune system. This prevents HIV from multiplying and can reduce the amount of HIV in the body.By attaching to the gp120 protein on the outer surface of HIV, fostemsavir blocks HIV from getting into and infecting the immune cells.
Fostemsavir is a prodrug, which means that it is an inactive drug. Once taken, a prodrug does not work until the body converts it into an active form. In the body, fostemsavir is converted to temsavir (also known as BMS-626529).
For research and scientific purpose only, not for human use.
Dasotraline(SEP-225289)|Supplied by DC Chemicals
Dasotraline(SEP-225289)|Supplied by DC Chemicals
Product name: Dasotraline(SEP-225289) |Cat No. DC8162|Other names: Dasotraline, SEP-225289|Cas: 675126-05-3|Molecule Weight: 291.05|Molecule Formular: C16H15Cl2N| Purity: >98%
For research and scientific purpose only, not for human use.
Product name: Dasotraline(SEP-225289) |Cat No. DC8162|Other names: Dasotraline, SEP-225289|Cas: 675126-05-3|Molecule Weight: 291.05|Molecule Formular: C16H15Cl2N| Purity: >98%
For research and scientific purpose only, not for human use.
Xeglyze(Abametapir)|Supplied by DC Chemicals
Xeglyze(Abametapir)|Supplied by DC Chemicals
Product name: Xeglyze(Abametapir) |Cat No. DC8161|Other names: Xeglyze, Abametapir|Cas: 1762-34-1|Molecule Weight: 184.1|Molecule Formular: C12H12N2| Purity: >98%
For research and scientific purpose only, not for human use.
Product name: Xeglyze(Abametapir) |Cat No. DC8161|Other names: Xeglyze, Abametapir|Cas: 1762-34-1|Molecule Weight: 184.1|Molecule Formular: C12H12N2| Purity: >98%
For research and scientific purpose only, not for human use.
ZGN-440(Beloranib)|MetAP2 inhibitor|DC Chemicals
ZGN-440(Beloranib)|MetAP2 inhibitor|DC Chemicals
Beloranib is being studied as a first-in-class obesity therapy that demonstrates a unique mechanism of action through methionine aminopeptidase 2 (MetAP2 ) inhibition.
Product name: ZGN-440(Beloranib) |Cat No. DC8160|Other names: ZGN-440，Beloranib，ZGN440|Cas: 251111-30-5|Molecule Weight: 499.65322|Molecule Formular: C29H41NO6| Purity: >98%
beloranib is a methionine aminopeptidase 2 (MetAP2) inhibitor.
For research and scientific purpose only, not for human use.
Beloranib is being studied as a first-in-class obesity therapy that demonstrates a unique mechanism of action through methionine aminopeptidase 2 (MetAP2 ) inhibition.
Product name: ZGN-440(Beloranib) |Cat No. DC8160|Other names: ZGN-440，Beloranib，ZGN440|Cas: 251111-30-5|Molecule Weight: 499.65322|Molecule Formular: C29H41NO6| Purity: >98%
beloranib is a methionine aminopeptidase 2 (MetAP2) inhibitor.
For research and scientific purpose only, not for human use.
L-701,324|NMDA receptor antagonist|DC Chemicals
L-701,324|NMDA receptor antagonist|DC Chemicals
L-701,324 is a selective antagonist at the glycine site of the NMDA receptor, counteracts haloperidol-induced muscle rigidity in rats.
Product name: L-701,324 |Cat No. DC8159|Other names: L-701,324,L-701324,L701324|Cas: 142326-59-8|Molecule Weight: 363.79|Molecule Formular: C21H14ClNO3| Purity: >98%
L-701,324 is a selective antagonist at the glycine site of the NMDA receptor, counteracts haloperidol-induced muscle rigidity in rats. L-701,324 exhibits a beneficial action in the animal model of parkinsonian rigidity, but not that of parkinsonian akinesia.L-701,324 (2.5-40 mg/kg IP) dose-dependently decreased the muscle tone enhanced by haloperidol (1-5 mg/kg IP). Likewise, the haloperidol-enhanced resting EMG activity and the EMG reflex response to passive movements were diminished by lower and almost abolished by higher doses of L-701,324. However, up to a dose of 20 mg/kg IP, L-701,324 did not influence haloperidol (0.5 mg/kg IP)-induced catalepsy. Moreover, L-701,324 (1.25-5 mg/kg IP) given alone or together with haloperidol (0.5-1 mg/kg IP) disturbed rotarod performance. Gross observation of behaviour indicated that rats injected with L-701,324 in doses equal to or higher than 5 mg/kg, alone or in combination with haloperidol, were markedly ataxic, i.e. rats showed signs of disturbed balance and loss of control over their hind limbs.
For research and scientific purpose only, not for human use.
L-701,324 is a selective antagonist at the glycine site of the NMDA receptor, counteracts haloperidol-induced muscle rigidity in rats.
Product name: L-701,324 |Cat No. DC8159|Other names: L-701,324,L-701324,L701324|Cas: 142326-59-8|Molecule Weight: 363.79|Molecule Formular: C21H14ClNO3| Purity: >98%
L-701,324 is a selective antagonist at the glycine site of the NMDA receptor, counteracts haloperidol-induced muscle rigidity in rats. L-701,324 exhibits a beneficial action in the animal model of parkinsonian rigidity, but not that of parkinsonian akinesia.L-701,324 (2.5-40 mg/kg IP) dose-dependently decreased the muscle tone enhanced by haloperidol (1-5 mg/kg IP). Likewise, the haloperidol-enhanced resting EMG activity and the EMG reflex response to passive movements were diminished by lower and almost abolished by higher doses of L-701,324. However, up to a dose of 20 mg/kg IP, L-701,324 did not influence haloperidol (0.5 mg/kg IP)-induced catalepsy. Moreover, L-701,324 (1.25-5 mg/kg IP) given alone or together with haloperidol (0.5-1 mg/kg IP) disturbed rotarod performance. Gross observation of behaviour indicated that rats injected with L-701,324 in doses equal to or higher than 5 mg/kg, alone or in combination with haloperidol, were markedly ataxic, i.e. rats showed signs of disturbed balance and loss of control over their hind limbs.
For research and scientific purpose only, not for human use.
PLX3397 (Pexidartinib)|CSF1 inhibitor|DC Chemicals
PLX3397 (Pexidartinib)|CSF1 inhibitor|DC Chemicals
PLX3397 is a tyrosine kinase inhibitor that potently inhibits the colony stimulating factor 1 (CSF1) receptor kinase, a driving force in the development and growth of PVNS.
Product name: Pexidartinib(PLX3397) |Cat No. DC8158|Other names: PLX3397,PLX 3397,PLX-3397,Pexidartinib|Cas: 1029044-16-3|Molecule Weight: 417.81|Molecule Formular: C20H15ClF3N5| Purity: >98%
In the study, 23 patients with advanced PVNS in a single joint received 1000 mg of PLX3397 orally each day. Patients underwent an MRI every two months to measure tumor volume using a novel tumor volume score developed for PVNS. Among the 14 patients with evaluable MRI scans, the mean tumor size reduction was 61 percent. Eleven patients experienced a partial response (at least a 50 percent decrease in tumor volume compared to baseline screenings) and three had stable disease. Patients remained on the drug until disease progression or intolerability.
For research and scientific purpose only, not for human use.
PLX3397 is a tyrosine kinase inhibitor that potently inhibits the colony stimulating factor 1 (CSF1) receptor kinase, a driving force in the development and growth of PVNS.
Product name: Pexidartinib(PLX3397) |Cat No. DC8158|Other names: PLX3397,PLX 3397,PLX-3397,Pexidartinib|Cas: 1029044-16-3|Molecule Weight: 417.81|Molecule Formular: C20H15ClF3N5| Purity: >98%
In the study, 23 patients with advanced PVNS in a single joint received 1000 mg of PLX3397 orally each day. Patients underwent an MRI every two months to measure tumor volume using a novel tumor volume score developed for PVNS. Among the 14 patients with evaluable MRI scans, the mean tumor size reduction was 61 percent. Eleven patients experienced a partial response (at least a 50 percent decrease in tumor volume compared to baseline screenings) and three had stable disease. Patients remained on the drug until disease progression or intolerability.
For research and scientific purpose only, not for human use.
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