2016年1月27日星期三

NS 11021|NS11021|cas 956014-19-0| DC Chemicals

NS 11021|NS11021|cas 956014-19-0| DC Chemicals

NS 11021 is an activator of large-conductance Ca2+-activated potassium channels (BKCa, KCa1.1). 

Product Name: NS 11021 |Catalog Number: DC8789 |CAS 956014-19-0 |Other names: NS11021,NS 11021,NS-11021 |Chemical Name: N'-[3,5-Bis(trifluoromethyl)phenyl]-N-[4-bromo-2-(2H-tetrazol-5-yl-phenyl]thiourea |Molecule Formular: C16H9BrF6N6S |MW: 511.24

Activator of large-conductance Ca2+-activated potassium channels (BKCa, KCa1.1). Exhibits no modulatory effect on a variety of K+ (KV), Na+ and Ca2+ currents at concentrations <10 μM. Alters gating kinetics, but does not affect single channel conductance. Shown to bind BKCa in open and closed conformations; thought to bind the α subunit.

For research only, not for human use!

Ko 143|Ko143|BCRP inhibitor| DC Chemicals

Ko 143|Ko143|BCRP inhibitor| DC Chemicals

Ko 143 is a potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM), Ko 143 displays > 200-fold selectivity over P-gp and MRP-1 transporters.

Product Name: Ko 143 |Catalog Number: DC8788 |CAS 461054-93-3 |Other names: Ko-143; Ko143 |Chemical Name:  |Molecule Formular: C26H35N3O5 |MW: 469.57

Ko 143 is a potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM), Ko 143 displays > 200-fold selectivity over P-gp and MRP-1 transporters.
in vitro:  Ko143 appears to be the most potent BCRP inhibitor known thus far. In contrast, the compounds have only low activity against P-glycoprotein, the multidrug resistance-associated protein (MRP1), or other known drug transporters.
in vivo: Ko 143 is nontoxic in vitro at useful concentrations and evinced no signs of toxicity in mice at high oral or i.p. doses. Administered p.o. to inhibit intestinal Bcrp1, Ko143 markedly increased the oral availability of topotecan in mice.

For research only, not for human use!



NQDI-1|ASK1 inhibitor| DC Chemicals

NQDI-1|ASK1 inhibitor| DC Chemicals

NQDI-1 is a specific inhibitor of ASK1 (IC50 = 3 μM; Ki = 500 nM) that demonstrates potent selectivity against various serine/threonine and tyrosine protein kinases.

Product Name: NQDI-1 |Catalog Number: DC8787 |CAS 175026-96-7 |Other names: NQDI-1,NQDI 1,NQDI1 |Chemical Name: 2,​7-​dihydro-​2,​7-​dioxo-3H-​naphtho[1,​2,​3-​de]​quinoline-​1-​carboxylic acid​, ethyl ester |Molecule Formular: C19H13NO4 |MW: 319.3

NQDI-1 is a specific inhibitor of ASK1 (IC50 = 3 μM; Ki = 500 nM) that demonstrates potent selectivity against various serine/threonine and tyrosine protein kinases. It has been used to promote survival of induced pluripotent stem cell populations and to protect neurons from reactive oxygen species-induced apoptosis in a model of ischemia.

For research only, not for human use!

NVP-BEZ235|cas 915019-65-7|supplier DC Chemicals

NVP-BEZ235|cas 915019-65-7|supplier DC Chemicals

BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively, and also inhibits ATR with IC50 of 21 nM.

Product Name: NVP-BEZ235 Tosylate |Catalog Number: DC8786 |CAS 1028385-32-1 |Other names: BEZ235 |Chemical Name: 2-methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl)phenyl)propanenitrile |Molecule Formular: C37H31N5O4S |MW: 641.74

Description of BEZ235: BEZ235 is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor BEZ235 specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane, increasing mitochondrial membrane permeability; apoptotic cell death may ensue. Bax is a member of the proapoptotic Bcl2 family of proteins. Check  For active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
 For the detailed information about the solubility of NVP-BEZ235 in water, the solubility of NVP-BEZ235 in DMSO, the solubility of NVP-BEZ235 in PBS buffer, the animal experiment(test) of NVP-BEZ235,the in vivo,in vitro and clinical trial test of NVP-BEZ235,the cell experiment(test) of NVP-BEZ235,the IC50, EC50 and Affinity of NVP-BEZ235, please contact DC Chemicals.

For research only, not for human use!


TC-O 9311|GPR139 agonist|DC Chemicals

TC-O 9311|GPR139 agonist|DC Chemicals

TC-O 9311 is an activator of GPR139.

Product Name: TC-O 9311 |Catalog Number: DC8785 |CAS 444932-31-4 |Other names:  |Chemical Name: 3,5-Dimethoxybenzoic acid 2-[(1-naphthalenylamino)carbonyl]hydrazide |Molecule Formular: C20H19N3O4 |MW: 365.38

Potent GPR139 agonist (EC50 = 39 nM in CHO-K1 cells expressing human GPR139). Displays no activity against a range of 90 diverse targets.

For research only, not for human use!

CTLA-4 inhibitor|CAS 635324-72-0|DC Chemicals

CTLA-4 inhibitor|CAS 635324-72-0|DC Chemicals

A novel CTLA-4 inhibitor.

Product Name: CTLA-4 inhibitor |Catalog Number: DC8784 |CAS 635324-72-0 |Other names:  |Chemical Name:  |Molecule Formular: C21H13F4N5O |MW: 427.11

For research only, not for human use!

NS 9283|NS9283|cas 913830-15-6|DC Chemicals

NS 9283|NS9283|cas 913830-15-6|DC Chemicals

NS 9283 is a positive allosteric modulator of α4β2 receptor; increases the potency of Ach-evoked currents ~60 fold without effecting the maximum efficacy (HEK293-hα4β2 cells). 

Product Name: NS 9283 |Catalog Number: DC8783 |CAS 913830-15-6 |Other names: NS 9283,NS-9283,NS9283 |Chemical Name: 3-[3-(3-Pyridinyl)-1,2,4-oxadiazol-5-yl]benzonitrile |Molecule Formular: C14H8N4O |MW: 248.24

NS 9283 is a positive allosteric modulator of α4β2 receptor; increases the potency of Ach-evoked currents ~60 fold without effecting the maximum efficacy (HEK293-hα4β2 cells). Reduces the rate of recovery from desensitization and slows the rate of deactivation. Displays a synergistic effect on the Emax when given with NS206 at 3α:2β receptors.

For research only, not for human use!

INCB032304|cas 941685-27-4|DC Chemicals

INCB032304|cas 941685-27-4|DC Chemicals

Product Name: INCB032304 |Catalog Number: DC8782 |CAS 941685-27-4 |Other names:  |Chemical Name:  |Molecule Formular: C15H21N5OSi |MW: 315.45

For research only, not for human use!

Flavopiridol Hydrochloride|cas 131740-09-5|DC Chemicals

Flavopiridol Hydrochloride|cas 131740-09-5|DC Chemicals

Flavopiridol hydrochloride competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA.

Product Name: Flavopiridol Hydrochloride |Catalog Number: DC8780 |CAS 131740-09-5 |Other names: HL 275;  NSC 649890;  MDL 107826A;  FLAVOPIRIDOL HCL;  Alvocidib Hydrochloride |Chemical Name:  |Molecule Formular: C21H21Cl2NO5 |MW: 438.3

Flavopiridol hydrochloride competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA.in vitro: Flavopiridol induces G1 arrest with inhibition of CDK2 and CDK4 in human breast carcinoma cells in a time and concentration dependent manner. Short time treatment of Flavopiridol (~12 hours) induce apoptosis in hematopoietic cell lines including SUDHL4, SUDHL6 (B-cell lines), Jurkat and MOLT4 (T-cell lines ), and HL60 (myeloid). In the clonogenic assay, Flavopiridol functions as a highly potent cytotoxic compound with a mean IC70 with 8 ng/mL in 23 human tumor models. A recent study shows Flavopiridol treatment induces a substantial AKT-Ser473 phosphorylation in human glioblastoma T98G cell line.in vivo: After treatment with 7.5 mg/kg Flavopiridol bolus intravenous (IV) or intraperitoneal on each of 5 consecutive days, 11 out of 12 advanced stage subcutaneous (s.c.) human HL-60 xenografts undergo complete regressions, and animals remain disease-free several months after one course of Flavopiridol treatment. SUDHL-4 s.c. lymphomas treated with flavopiridol at 7.5 mg/kg bolus IV for 5 days undergo either major (two out of eight mice) or complete (four out of eight mice) regression, with two animals remaining disease-free for more than 60 days. The overall growth delay is 73.2%.

For research only, not for human use!




Glycopyrrolate|cas 596-51-0|DC Chemicals

Glycopyrrolate|cas 596-51-0|DC Chemicals

Glycopyrrolate(Glycopyrronium Br) is a muscarinic competitive antagonist used as an antispasmodic.

Product Name: Glycopyrrolate |Catalog Number: DC8779 |CAS 596-51-0 |Other names: Glycopyrrolate bromide; Glycopyrronium bromide |Chemical Name:  |Molecule Formular: C19H28BrNO3 |MW: 398.33

Glycopyrrolate(Glycopyrronium Br) is a muscarinic competitive antagonist used as an antispasmodic.in vitro: Glycopyrrolate showed no selectivity in its binding to the M1-M3 receptors. Kinetics studies, however, showed that glycopyrrolate dissociates slowly from HASM muscarinic receptors (60% protection against [3H]-NMS binding at 30 nM) compared to ipratropium bromide.
in vivo: Glycopyrrolate (1 mg) tablets were then administered, starting with one tablet daily the third week and increasing the daily dose by one tablet per week until a maximum of four tablets during week six and 4 days of week seven when the daily dose was reduced to two tablets for 3 days. glycopyrrolate can be given in controlled doses provided that an adequate medical assessment has been undertaken. Glycopyrrolate has a slow and erratic absorption from the gastrointestinal system, but even low plasma levels are associated with a distinct and long-lasting antisialogic effect. Oral glycopyrrolate is emerging as a potential second-line treatment option, but experience with safety, efficacy, and dosing is especially limited in children. phase III study, 52.3% of glycopyrrolate oral solution recipients (aged 3-18 years; n = 137) had an mTDS response (primary endpoint); the response rate was consistently above 50% at all 4-weekly timepoints, aside from the first assessment at week 4 (40.3%). In general, glycopyrrolate oral solution was well tolerated in clinical trials. The majority of adverse events were within expectations as characteristic anticholinergic outcomes.

For research only, not for human use!


Enocitabine|cas 55726-47-1|DC Chemicals

Enocitabine|cas 55726-47-1|DC Chemicals

Enocitabine is an anti-tumor agent and an antineoplastic. A derivative of Cytarabine.

Product Name: Enocitabine |Catalog Number: DC8778 |CAS 55726-47-1 |Other names: Sunrabin; |Chemical Name:  |Molecule Formular: C31H55N3O6 |MW: 565.78

Enocitabine is an anti-tumor agent and an antineoplastic. A derivative of Cytarabine.

For research only, not for human use!

CEP-32496 hydrochloride|cas 1227678-26-3|DC Chemicals

CEP-32496 hydrochloride|cas 1227678-26-3|DC Chemicals

CEP-32496 Hcl is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2.

Product Name: CEP-32496 hydrochloride |Catalog Number: DC8777 |CAS 1227678-26-3 |Other names: CEP 32496 hydrochloride; CEP32496 hydrochloride |Chemical Name:  |Molecule Formular: C24H23ClF3N5O5 |MW: 553.92

CEP-32496 Hcl is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2.CEP-32496 is a potent BRAF inhibitor in an in vitro binding assay for mutated BRAF(V600E) (K(d) BRAF(V600E) = 14 nM) and in a mitogen-activated protein (MAP)/extracellular signal-regulated (ER) kinase (MEK) phosphorylation (pMEK) inhibition assay in human melanoma (A375) and colorectal cancer (Colo-205) cell lines (IC(50) = 78 and 60 nmol/L). In vitro, CEP-32496 has multikinase binding activity at other cancer targets of interest; however, it exhibits selective cellular cytotoxicity for BRAF(V600E) versus wild-type cells.

For research only, not for human use!

CCT 137690|cas 1095382-05-0|DC Chemicals

CCT 137690|cas 1095382-05-0|DC Chemicals

CCT 137690 is a potent inhibitor of Aurora kinases (IC50 values are 0.015, 0.019 and 0.025 μM at Aurora A, Aurora C and Aurora B respectively).

Product Name: CCT 137690 |Catalog Number: DC8776 |CAS 1095382-05-0 |Other names: CCT-137690; CCT137690 |Chemical Name:  |Molecule Formular: C26H31BrN8O |MW: 551.48

CCT 137690 is a potent inhibitor of Aurora kinases (IC50 values are 0.015, 0.019 and 0.025 μM at Aurora A, Aurora C and Aurora B respectively).in vitro: CCT137690 displays antiproliferative activity in a range of human tumor cell lines, including SW620 colon carcinoma cell and A2780 ovarian cancer cell with GI50 of 0.3 and o.14 μM, respectively. In addition, CCT137690 also inhibit the phosphorylation of histone H3. CCT137690 inhibits the major cytochrome P450 isoforms (CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP3A4) with IC50 greater than 10 μM. However, CCT137690 is a moderate inhibitor of the hERG ion-channel with IC50 of 3.0 μM. CCT137690 inhibits autophosphorylation of FLT3 and phosphorylation of its downstream targets STAT5 and p44/42 MAPK (Erk1/2). CCT137690 effectively inhibits the growth of human tumor cell lines of different origins with GI50 ranging from 0.005 to 0.47 μM. CCT137690 completely inhibits both Aurora A autophosphorylation at T288 and histone H3 phosphorylation at 0.5 μM. CCT137690 induces polyploidy, mitotic aberrations, and apoptosis in HCT116 cells. CCT137690 reduces MYCN levels and GSK3β phosphorylation in the KELLY neuroblastoma cell line.
in vivo: CCT137690 inhibits growth of MYCN-induced neuroblastoma at a dose of 100 mg/kg. Additionally, CCT137690 achieves target modulation and potently inhibits the growth of subcutaneous MOLM-13 xenografts, with no obvious toxicity or loss of body weight. CCT137690 is highly orally bioavailable and inhibits the growth of SW620 colon carcinoma xenografts with no observed toxicities as defined by body weight loss.

For research only, not for human use!


LED209|cas 245342-14-7|DC Chemicals

LED209|cas 245342-14-7|DC Chemicals

LED209 is a potent QseC inhibitor that blocks both norepinephrine- and epinephrine-triggered QseC-dependent virulence gene expression at 5 pM in vitro.

Product Name: LED209 |Catalog Number: DC8775 |CAS 245342-14-7 |Other names:  |Chemical Name:  |Molecule Formular: C19H17N3O2S2 |MW: 383.49

LED209 is a potent QseC inhibitor that blocks both norepinephrine- and epinephrine-triggered QseC-dependent virulence gene expression at 5 pM in vitro.

For research only, not for human use!

KPT251|cas 1388841-50-6|DC Chemicals

KPT251|cas 1388841-50-6|DC Chemicals

Product Name: KPT251 |Catalog Number: DC8774 |CAS 1388841-50-6 |Other names: SCHEMBL11318201; AOB6639;  |Chemical Name:  |Molecule Formular: C14H7F6N5O |MW: 375.23

For research only, not for human use!

JNJ-7777120|cas 459168-41-3|DC Chemicals

JNJ-7777120|cas 459168-41-3|DC Chemicals

JNJ-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, exhibits >1000-fold selectivity over the other histamin receptors.

Product Name: JNJ-7777120 |Catalog Number: DC8773 |CAS 459168-41-3 |Other names: JNJ7777120 |Chemical Name:  |Molecule Formular: C14H16ClN3O |MW: 277.75

JNJ-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, exhibits >1000-fold selectivity over the other histamin receptors.in vitro: JNJ-7777120 prevents fibronectin-induced lung fibroblast migration, thus suggesting that H4R could represent an attractive target for the development of new drugs for lung fibrosis treatment .
in vivo: JNJ 7777120 blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells. In addition, it can block the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice. JNJ 7777120 significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model.

For research only, not for human use!

Isradipine|cas 75695-93-1|DC Chemicals

Isradipine|cas 75695-93-1|DC Chemicals

Isradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.

Product Name: Isradipine |Catalog Number: DC8772 |CAS 75695-93-1 |Other names: PN 200-110;DynaCirc; Lomir; Prescal; Dynacirc CR; |Chemical Name:  |Molecule Formular: C19H21N3O5 |MW: 371.39

Isradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.Isradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.It is usually prescribed for the treatment of high blood pressure in order to reduce the risk of stroke and heart attack. Isradipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. It is structurally related to felodipine, nifedipine, and nimodipine and is the most potent calcium-channel blocking agent of the DHP class. Isradipine binds to calcium channels with high affinity and specificity and inhibits calcium flux into cardiac and arterial smooth muscle cells. It exhibits greater selectivity towards arterial smooth muscle cells owing to alternative splicing of the alpha-1 subunit of the channel and increased prevalence of inactive channels in smooth muscle cells. Isradipine may be used to treat mild to moderate essential hypertension.

For research only, not for human use!

Irbinitinib|cas 937263-43-9|DC Chemicals

Irbinitinib|cas 937263-43-9|DC Chemicals

Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.

Product Name: Irbinitinib |Catalog Number: DC8771 |CAS 937263-43-9 |Other names: ARRY-380;Irbinitinib [INN]; SCHEMBL1193050; ONT-380; |Chemical Name:  |Molecule Formular: C26H24N8O2 |MW: 480.52

For research only, not for human use!

IMD-0354|cas 978-62-1|DC Chemicals

IMD-0354|cas 978-62-1|DC Chemicals

IMD-0354 is a synthetic selective NF-kB inhibitor.

Product Name: IMD-0354 |Catalog Number: DC8770 |CAS 978-62-1 |Other names: IKK-2 Inhibitor V; IMD 0354;IMD0354; |Chemical Name:  |Molecule Formular: C15H8ClF6NO2 |MW: 383.67

IMD-0354 is a synthetic selective NF-kB inhibitor.in vitro: IMD-0354 inhibits p65 translocation to the nucleus promoted by FGF2 in PASMCs. Furthermore, the time courses of Erk1/2, MCP-1, and PAI-1 stimulated with FGF2 are each markedly shortened by IMD-0354. IMD-0354 suppresses proliferation and induced apoptosis of PASMCs. IMD-0354 decreases FGF2, PAI-1, t-PA mRNA expressions. IMD-0354 also inhibits the translocation of NF-kB subunit p65 into the nucleus.in vivo: IMD-0354 has potential as a new therapeutic tool for PAH. IMD-0354 improves survival in the PAH rats. IMD-0354 improves physical signs of RVH in the PAH rats. IMD-0354 also decreases medial hypertrophy in the pulmonary arterioles.

For research only, not for human use!

IEM 1754 DihydrobroMide|cas 162831-31-4|DC Chemicals

IEM 1754 DihydrobroMide|cas 162831-31-4|DC Chemicals

IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.

Product Name: IEM 1754 DihydrobroMide |Catalog Number: DC8769 |CAS 162831-31-4 |Other names:  IEM1754 dihydrobromide;IEM1754 2 HBr; AOB5933; |Chemical Name:  |Molecule Formular: C16H32Br2N2 |MW: 412.25

IEM 1754 is an adamantane derivative. IEM 1754 causes use- and voltage-dependent block of open channels of recombinant AMPA receptors. This antagonism is dependent on receptor subunit composition, channels gated by recombinant, homomeric GluR1 and GluR3 receptors exhibites a higher sensitivity to block than those gated by receptors containing edited GluR2 subunits.IEM-1754 block of GluR2-containing AMPAR is enhanced by hyperpolarization in agreement with the classical single-exponential model. In contrast, the block of GluR2-lacking AMPAR is reduced by hyperpolarization.

For research only, not for human use!

HMN-214|cas 173529-46-9|DC Chemicals

HMN-214|cas 173529-46-9|DC Chemicals

HMN-214(IVX214) is a potent PLK1 inhibitor an average IC50 of 0.12 μM.

Product Name: HMN-214 |Catalog Number: DC8768 |CAS 173529-46-9 |Other names: IVX-214; HMN214; HMN 214; IVX 214; IVX-214; IVX214 |Chemical Name:  |Molecule Formular: C22H20N2O5S |MW: 424.47

HMN-214(IVX214) is a potent PLK1 inhibitor an average IC50 of 0.12 μM.in vitro: HMN-214 is an oral prodrug that is rapidly converted to HMN-176. The in vitro data of HMN-214 are scarce. However, HMN-176, active metabolite of HMN-214, shows potent and broad-spectrumanti-tumor activity against various cancer cells, including HeLa, PC-3, DU-145, MIAPaCa-2, U937, MCF-7, A549, and WiDr, with a mean IC50 value of 118 nM. HMN-176 is also cytotoxic to drug-resistant human and murine cell lines, including P388/CDDP, P388/VCR, K2/CDDP, and K2/VP-16, with IC50 values ranging from 143 nM–265 nM. In HeLa cells, HMN-176 (3 μM) blocks cell cycle at G2/M phase. In Doxorubicin-resistant K2/ARS cells, HMN-176 inhibits cell growth with an IC50 value of 2 μM. HMN-176 (3 μM) down-regulates the expression of the multidrug resistance gene (MDR1), due to the disturbance of NF-Y transcription factor binding to the MDR1 promoter. In human RPE1 and CFPAC-1 cells, HMN-176 (2.5 μM) delays satisfaction of the spindle assembly checkpoint. HMN-176 (250 nM–2.5 μM) inhibits meiotic spindle assembly and aster formationin Spisula oocytes. HMN-176 (2.5 μM) also inhibits aster microtubule formation from human centrosomes. These results indicate that the anti-tumor activity of HMN-176 is at least partially via disrupting centrosome-mediated MT assembly during mitosis.
in vivo: HMN-214 is an oral pro-drug of HMN-176 with improved oral absorption. HMN-214 (30 mg/kg) triggers no obvious neurotoxicity in mice. In mouse xenograft model of PC-3, A549, and WiDr cells, HMN-214 (10 mg/kg–20 mg/kg) inhibits tumor growth. In nude mice model bearing multidrug-resistant KB-A.1 cells, HMN-214 (10 mg/kg–20 mg/kg) significantly suppresses MDR1 mRNA expression.

For research only, not for human use!


GSK256066|cas 801312-28-7|DC Chemicals

GSK256066|cas 801312-28-7|DC Chemicals

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.

Product Name: GSK256066 |Catalog Number: DC8767 |CAS 801312-28-7 |Other names: GSK-256066; GSK 256066 |Chemical Name:  |Molecule Formular: C27H26N4O5S |MW: 518.58

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.in vitro: GSK256066 is a slow and tight binding inhibitor of PDE4B with apparent IC50 of 3.2 pM. GSK256066 is an extremely potent inhibitor of LPS-stimulated TNFα production in PBMCs with pIC50 of 11.0 and IC50 of 10 pM and human whole-blood cultures with pIC50 of 9.90 and IC50 of 126 pM. GSK256066 is highly selective for PDE4 (>3.8 × 105-fold versus PDE1, PDE2, PDE3, PDE5, and PDE6 and >2.5 × 103-fold against PDE7). GSK256066 inhibits PDE4 isoforms A-D with equal affinity.
in vivo: GSK256066 inhibits the LPS-induced pulmonary neutrophilia with an ED50 of 1.1 μg/kg, achieving maximal inhibition of 72% at 30 μg/kg when given in the aqueous suspension. GSK256066 inhibits the LPS-induced pulmonary neutrophilia with ED50 of 2.9 μg/kg, achieving maximal inhibition of 62% when given in the dry powder formulation. GSK256066 shows a moderate plasma clearance of 39 ml/min/kg, a moderate volume of distribution of 0.8 L/kg, and a relatively short half-life of 1.1 hour in the male CD rat. GSK256066 sustains at a high lung concentration of 2.6 μg/g after intra-tracheal administration as an aqueous suspension at a dose of 30 μg/kg in rats.  GSK256066 (10 μg/kg) is administered intratracheally at different times (2, 6, 12, 18, 24, and 36 hours) before LPS administration, inhibiting LPS-Induced Pulmonary Neutrophilia in rat lipopolysaccharide (LPS)-induced models of acute pulmonary inflammation. GSK256066 (0.3–100 μg/kg) inhibits LPS-induced increases in exhaled nitric oxide with ED50 of 35 μg/kg in rat. GSK256066 (10 μg/kg) is administered half a hour before OVA administration in rat, inhibiting OVA-induced pulmonary eosinophilia with ED50 of 0.4 μg/kg. GSK256066 administered intratracheally as a dry powder blended in respiratory-grade lactose at doses of 3 to 100 μg/kg 2 hours before inhaled LPS challenge in ferrets, inhibiting LPS-induced pulmonary neutrophilia with ED50 of 18 μg/kg without inducing emetic episodes.

For research only, not for human use!


GSK1324726A|cas 1300031-52-0|DC Chemicals

GSK1324726A|cas 1300031-52-0|DC Chemicals

GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM).

Product Name: GSK1324726A |Catalog Number: DC8766 |CAS 1300031-52-0 |Other names: I-BET726; GSK 1324726A; GSK-1324726A; I-BET 726 |Chemical Name:  |Molecule Formular: C25H23ClN2O3 |MW: 434.91

GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM).in vitro: I-BET726 is a novel small molecule inhibitor that binds to the acetyl-lysine recognition pocket of BET family proteins. It binds with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM), and competes with tetra-acetylated histone H4 peptides (K5ac, K8ac, K12ac, K16ac) for binding to the bromodomains of these proteins. I-BET726 is highly selective for BET family proteins, exhibiting no binding affinity for any bromodomain-containing homolog tested with the exception of CREBBP, for which I-BET726 binds with >1000-fold lower affinity than to BET family proteins. Since potent anti-proliferative activity was observed for BET inhibitors in MYC-driven hematologic cancer models, we screened a panel of neuroblastoma cell lines, in which MYCN amplification is common, for effects on cell growth following I-BET726 treatment. All neuroblastoma cell lines tested exhibited potent growth inhibition, with a median growth IC50 value (gIC50; inhibitor concentration resulting in 50% growth inhibition) equal to 75 nM. I-BET726 modulates expression of genes involved in apoptosis, signaling, and MYC-family pathways. I-BET726 directly regulates expression of BCL2.
in vivo: I-BET726 was administered by oral gavage once daily at doses of 5 mg/kg or 15 mg/kg. Blood and tumor concentrations of I-BET726 were comparable between the two models, confirming that a similar exposure was achieved in the two studies. In the CHP-212 model, treatment with 5 mg/kg I-BET726 resulted in TGI equal to 50% (n=8; p= 0.1816), and mice in the 15 mg/kg group exhibited a TGI of 82% at the end of the study (n=5; p =0.0488).

For research only, not for human use!

AM251|cas 183232-66-8|DC Chemicals

AM251|cas 183232-66-8|DC Chemicals

AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also potent GPR55 agonist (EC50 = 39 nM).

Product Name: AM251 |Catalog Number: DC8765 |CAS 183232-66-8 |Other names: AM-251 |Chemical Name:  |Molecule Formular: C22H21Cl2IN4O |MW: 555.24

AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also potent GPR55 agonist (EC50 = 39 nM).in vitro: In in vitro binding assays with mouse hippocampal membranes, tetrahydrocannabinol inhibited binding of [123I]AM251 with an IC50 value of about 700 nM, compared with about 0.2 nM for SR141716A. Kd values were lower for [123I]AM251 (0.23-0.62 nM) than for [3H]CP 55,940 (1.3-4 nM). CP 55,940 and SR141716A increased dissociation of [123I]AM251 from binding sites in mouse cerebellar homogenates to a similar extent.

For research only, not for human use!

AR 231453|cas 733750-99-7|DC Chemicals

AR 231453|cas 733750-99-7|DC Chemicals

AR231453 is a potent and selective small molecule agonist of GPR119 that enhances glucose-dependent insulin secretion and glucagon-like peptide 1 (GLP-1) release; Antidiabetic agent.

Product Name: AR 231453 |Catalog Number: DC8764 |CAS 733750-99-7 |Other names: AR231453; AR-231453 |Chemical Name:  |Molecule Formular: C21H24FN7O5S |MW: 505.52

AR231453 is a potent and selective small molecule agonist of GPR119 that enhances glucose-dependent insulin secretion and glucagon-like peptide 1 (GLP-1) release; Antidiabetic agent.in vitro: The GPR119-specific agonist AR231453 significantly increased cAMP accumulation and insulin release in both HIT-T15 cells and rodent islets. In both cases, loss of GPR119 rendered AR231453 inactive. In GLUTag cells, a well-established model of intestinal L-cell function, the potent GPR119 agonist AR231453 stimulated cAMP accumulation and GLP-1 release.
in vivo: AR231453 also enhanced glucose-dependent insulin release in vivo and improved oral glucose tolerance in wild-type mice but not in GPR119-deficient mice. Diabetic KK/A(y) mice were also highly responsive to AR231453. Orally active GPR119 agonists may offer significant promise as novel antihyperglycemic agents acting in a glucose-dependent fashion. When administered in mice, AR231453 increased active GLP-1 levels within 2 min after oral glucose delivery and substantially enhanced total glucose-dependent insulinotropic peptide levels. Blockade of GLP-1 receptor signaling with exendin(9-39) reduced the ability of AR231453 to improve glucose tolerance in mice.

For research only, not for human use!


ARRY-380|cas 937265-83-3|DC Chemicals

ARRY-380|cas 937265-83-3|DC Chemicals

ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.

Product Name: ARRY-380 |Catalog Number: DC8763 |CAS 937265-83-3 |Other names: ARRY380; ARRY 380 |Chemical Name:  |Molecule Formular: C29H27N7O4S |MW: 569.63

ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.ErbB-2 inhibitor ARRY-380 selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. ErbB-2 is overexpressed in a variety of cancers and plays an important role in cellular proliferation and differentiation.

For research only, not for human use!

BMS-265246|cas 582315-72-8|DC Chemicals

BMS-265246|cas 582315-72-8|DC Chemicals

BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively.

Product Name: BMS-265246 |Catalog Number: DC8762 |CAS 582315-72-8 |Other names: BMS265246; BMS 265246 |Chemical Name:  |Molecule Formular: C18H17F2N3O2 |MW: 345.34

BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively.in vitro: BMS-265246 inhibits the activity of Cdk4/cycD (IC50 = 0.23 μM) and prevents A2780 Cytox with IC50 of 0.76 μM. BMS-265246 when bound to Cdk2, shows the inhibitor resides within the ATP purine binding site and forms important H-bonds with Leu83 on the protein backbone. BMS-265246 represents the most potent Cdk/Cdk2 selective analogue from this chemotype. A recent study shows that BMS-265246 inhibits cell proliferation with EC50 ranging from 0.293 μM-0.492 μM in HCT-116 cells. After treatment of BMS-265246, the dominant cell populations are G2-arrested cells having 4N DNA content, large round nuclei, and low DNA intensity.

For research only, not for human use!

BMS-345541|cas 547757-23-3|DC Chemicals

BMS-345541|cas 547757-23-3|DC Chemicals

BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.

Product Name: BMS-345541 |Catalog Number: DC8761 |CAS 547757-23-3 |Other names: BMS345541 hydrochloride; BMS-345541 hydrochloride; BMS 345541 hydrochloride |Chemical Name:  |Molecule Formular: C14H18ClN5 |MW: 291.78

BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.in vitro: BMS-345541 dose-dependently inhibits the TNF-α-stimulated phosphorylation of IκBα in THP-1 monocytic cells with an IC50 of ~4 μM. BMS-345541 inhibits lipopolysaccharide-stimulated tumor necrosis factorα, interleukin-1β, interleukin-8, and interleukin-6 in THP-1 cells with IC50 values in the 1- to 5 μM range. BMS-345541 binds in a mutually exclusive manner with respect to a peptide inhibitor corresponding to amino acids 26 - 42 of IκBα with Ser-32 and Ser-36 changed to aspartates and in a non-mutually exclusive manner with respect to ADP. BMS-345541 binds to similar allosteric sites on IKK-1 and IKK-2, which then affects the active sites of the subunits differently. BMS-345541 (10 μM) inhibits growth of Normal human epidermal melanocytes, and metastatic melanoma cells (SK-MEL-5, A375, and Hs 294T) by 96% and 99% at 72h, respectively. Application of 100 μM of BMS-345541 to SK-MEL-5 cell culture results in 87% apoptotic cells at 24 h through caspase-independent and AIF-dependent mitochondria-mediated manner. BMS-345541 treatment (10 μM) results in 76% and 95% reduction in IKK activities and NF-kB activity, as well as CXCL1 production. BMS-345541 inhibits the TNFα-induced expression of both ICAM-1 and VCAM-1 in human umbilical vein endothelial cells with IC50 of 5 μM.
in vivo: BMS-345541 effectively inhibits melanoma tumor growth in a dose-dependent manner. Tumor-bearing mice treated with 75 mg/kg of BMS-345541 shows effective inhibition of growth of SK-MEL-5, A375, and Hs 294T tumors by 86 %, 69% and 67%, respectively, when compared with control animals treated with vehicle alone.

For research only, not for human use!



2016年1月26日星期二

BMS-345541|cas 547757-23-3|DC Chemicals

BMS-345541|cas 547757-23-3|DC Chemicals

BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.

Product Name: BMS-345541 |Catalog Number: DC8761 |CAS 547757-23-3 |Other names: BMS345541 hydrochloride; BMS-345541 hydrochloride; BMS 345541 hydrochloride |Chemical Name:  |Molecule Formular: C14H18ClN5 |MW: 291.78

BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.in vitro: BMS-345541 dose-dependently inhibits the TNF-α-stimulated phosphorylation of IκBα in THP-1 monocytic cells with an IC50 of ~4 μM. BMS-345541 inhibits lipopolysaccharide-stimulated tumor necrosis factorα, interleukin-1β, interleukin-8, and interleukin-6 in THP-1 cells with IC50 values in the 1- to 5 μM range. BMS-345541 binds in a mutually exclusive manner with respect to a peptide inhibitor corresponding to amino acids 26 - 42 of IκBα with Ser-32 and Ser-36 changed to aspartates and in a non-mutually exclusive manner with respect to ADP. BMS-345541 binds to similar allosteric sites on IKK-1 and IKK-2, which then affects the active sites of the subunits differently. BMS-345541 (10 μM) inhibits growth of Normal human epidermal melanocytes, and metastatic melanoma cells (SK-MEL-5, A375, and Hs 294T) by 96% and 99% at 72h, respectively. Application of 100 μM of BMS-345541 to SK-MEL-5 cell culture results in 87% apoptotic cells at 24 h through caspase-independent and AIF-dependent mitochondria-mediated manner. BMS-345541 treatment (10 μM) results in 76% and 95% reduction in IKK activities and NF-kB activity, as well as CXCL1 production. BMS-345541 inhibits the TNFα-induced expression of both ICAM-1 and VCAM-1 in human umbilical vein endothelial cells with IC50 of 5 μM.
in vivo: BMS-345541 effectively inhibits melanoma tumor growth in a dose-dependent manner. Tumor-bearing mice treated with 75 mg/kg of BMS-345541 shows effective inhibition of growth of SK-MEL-5, A375, and Hs 294T tumors by 86 %, 69% and 67%, respectively, when compared with control animals treated with vehicle alone.

For research only, not for human use!


Acalisib|cas 870281-34-8|DC Chemicals

Acalisib|cas 870281-34-8|DC Chemicals

Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM.

Product Name: Acalisib |Catalog Number: DC8760 |CAS 870281-34-8 |Other names: UNII-OVW60IDW1D;Acalisib (GS-9820);  |Chemical Name:  |Molecule Formular: C21H16FN7O |MW: 401.4

Acalisib (GS-9820) inhibits the activity of PI3K, thereby preventing the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3), which decreases tumor cell proliferation and induces cell death. Wortmannin, LY294002, GDC0941, IC87114 and Acalisib induced a dramatic retraction of osteoclasts within 15-20 min to 65-75% of the initial area. In contrast, there was no significant retraction in response to vehicle, PIK75, TGX221 or AS252424. Moreover, wortmannin and Acalisib (GS-9820), but not PIK75 or TGX221, disrupted actin belts. Whereas PIK75, TGX221, and Acalisib had no significant effect on basal survival, all blocked RANKL-stimulated survival. PI3K-mediated signaling is often dysregulated in cancer cells; the targeted inhibition of PI3K is designed to preserve PI3K signaling in normal, non-neoplastic cells.

For research only, not for human use!

Thiamet G|cas 1009816-48-1|DC Chemicals

Thiamet G|cas 1009816-48-1|DC Chemicals

Thiamet G is a potent and selective inhibitor of O-GlcNAcase that demonstrates a Ki value of 21 nM.

Product Name: Thiamet G |Catalog Number: DC8759 |CAS 1009816-48-1 |Other names: Thiamet-G |Chemical Name:  |Molecule Formular: C9H16N2O4S |MW: 248.3

Thiamet G is a potent and selective inhibitor of O-GlcNAcase that demonstrates a Ki value of 21 nM.Thiamet G increases cellular O-GlcNAc-modified protein levels (EC50 = 30 nM) and blocks phosphorylation of tau protein both in cultured PC-12 cells and in rats (200 mg/kg/day). Thiamet G is the first highly potent O-GlcNAcase inhibitor known to be orally bioavailable and effectively cross the blood brain barrier.

For research only, not for human use!

Tipiracil hydrochloride|cas 183204-72-0|DC Chemicals

Tipiracil hydrochloride|cas 183204-72-0|DC Chemicals

Tipiralacil, also known as TPI,  is a thymidine phosphorylase inhibitor (TPI). Tipiracil is one of the active components in TAS-102, which is an anticancer drug candidate currently in clinical trials.

Product Name: Tipiracil hydrochloride |Catalog Number: DC8758 |CAS 183204-72-0 |Other names: Tipiracil |Chemical Name:  |Molecule Formular: C9H12Cl2N4O2 |MW: 279.12

Tipiralacil, also known as TPI,  is a thymidine phosphorylase inhibitor (TPI). Tipiracil is one of the active components in TAS-102, which is an anticancer drug candidate currently in clinical trials.TAS-102 is an antitumor agent composed of a combination of trifluorothymidine (FTD), a nucleoside that incorporates into DNA and inhibits a variety of genetic functions required for the proliferation of cancer cells, and tipiracil hydrochloride (TPI), an inhibitor of thymidine phosphorylase (which degrades FTD) that maintains an effective blood concentration of FTD. Tipiracil protects trifluridine from being broken down when taken orally.

For research only, not for human use!

Triciribine|cas 35943-35-2|DC Chemicals

Triciribine|cas 35943-35-2|DC Chemicals

Triciribine(API-2; NSC 154020) is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase.

Product Name: Triciribine |Catalog Number: DC8757 |CAS 35943-35-2 |Other names: API-2;  NSC 154020;  TCN |Chemical Name:  |Molecule Formular: C13H16N6O4 |MW: 320.3

Triciribine(API-2; NSC 154020) is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase.Triciribine, also known as API-2, suppresses the phosphorylation level and kinase activity of Akt. Triciribine is a cell-permeable tricyclic nucleoside that inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3. Triciribine does not inhibit PI3-Kinase or PDK1, the direct upstream activators of Akt, nor does it inhibit PKC, PKA, ERK1/2, serum- and glucocorticoid-inducible kinase, p38, STAT3, or JNK signalling pathways. Triciribine induces apoptosis and growth arrest in vitro, preferentially in human cancer cells with elevated levels of Akt. Triciribine potently and selectively inhibits growth of Akt-overexpressing tumors in mice. Triciribine also inhibits DNA synthesis and displays antiviral activity against HIV-1 and -2.

For research only, not for human use!

UNC2881|cas 1493764-08-1|DC Chemicals

UNC2881|cas 1493764-08-1|DC Chemicals

UNC2881 is a potent and specific Mer kinase inhibitor; inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM.

Product Name: UNC2881 |Catalog Number: DC8756 |CAS 1493764-08-1 |Other names: UNC 2881; UNC-2881 |Chemical Name:  |Molecule Formular: C25H33N7O2 |MW: 463.58

UNC2881 is a potent and specific Mer kinase inhibitor; inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM.Treatment with UNC2281 is also sufficient to block EGF-mediated stimulation of a chimeric receptor containing the intracellular domain of Mer fused to the extracellular domain of EGFR. In addition, UNC2881 potently inhibits collagen-induced platelet aggregation, suggesting that this class of inhibitors may have utility for prevention and/or treatment of pathologic thrombosis.,

For research only, not for human use!

WAY 100635 Hydrochloride|cas 146714-97-8|DC Chemicals

WAY 100635 Hydrochloride|cas 146714-97-8|DC Chemicals

Product Name: WAY 100635 Hydrochloride |Catalog Number: DC8755 |CAS 146714-97-8 |Other names: CHEMBL514874; |Chemical Name:  |Molecule Formular: C25H35ClN4O2 |MW: 459.024

For research only, not for human use!

Voxtalisib (SAR245409, XL765)|cas 1123889-87-1|DC Chemicals

Voxtalisib (SAR245409, XL765)|cas 1123889-87-1|DC Chemicals

Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. 

Product Name: Voxtalisib (SAR245409, XL765) |Catalog Number: DC8754 |CAS 1123889-87-1 |Other names: SAR245409 |Chemical Name:  |Molecule Formular: C31H29N5O6S |MW: 599.66

Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. 

For research only, not for human use!

Articaine hydrochloride|cas 23964-57-0|DC Chemicals

Articaine hydrochloride|cas 23964-57-0|DC Chemicals

Articaine Hydrochloride is a dental local anesthetic.

Product Name: Articaine hydrochloride |Catalog Number: DC8753 |CAS 23964-57-0 |Other names: Carticaine hydrochloride; Septanest hydrochloride; Ultracain hydrochloride |Chemical Name:  |Molecule Formular: C13H21ClN2O3S |MW: 320.84

Articaine Hydrochloride is a dental local anesthetic.Articaine Hydrochloride is a dental local anesthetic. Articaine: VAS (Visual Analogue Scale) scores (from 0 to 10 cm) by patients 4 to < 13 years of age are 0.5 for simple procedures and 1.1 for complex procedures, and average investigator scores are 0.4 and 0.6 for simple and complex procedures, respectively. No serious adverse events related to the articaine occurres, the only adverse event considered related to articaine is accidental lip injury in one patient. Articaine results in success rate of 64.5% in electronic pulp testing in healthy adult volunteers injected with 4% articaine. Articaine infiltration produces significantly more episodes of no response to maximum stimulation in first molars than lidocaine. Mandibular buccal infiltration is more effective with 4% articaine with epinephrine compared to 2% lidocaine with epinephrine. Articaine formulation results in successful pulpal anesthesia ranged from 75 to 92 percent and onset of pulpal anesthesia ranged from 4.2 to 4.7 minutes in healthy volunteer. For articaine, 4 percent (two of 56) of the subjects reported swelling and no subjects reported bruising. Ninety-eight percent (59 of 60) of the subjects had lip numbness with the articaine solution.

For research only, not for human use!

Regadenoson|cas 313348-27-5|DC Chemicals

Regadenoson|cas 313348-27-5|DC Chemicals

Regadenoson is the first selective A2A receptor agonist that is approved by the FDA and is currently used clinically.

Product Name: Regadenoson |Catalog Number: DC8752 |CAS 313348-27-5 |Other names: Lexiscan; CVT-3146; |Chemical Name:  |Molecule Formular: C15H18N8O5 |MW: 390.35

Regadenoson is the first selective A2A receptor agonist that is approved by the FDA and is currently used clinically.

For research only, not for human use!

Licofelone|cas 156897-06-2|DC Chemicals

Licofelone|cas 156897-06-2|DC Chemicals

Licofelone is a dual COX/LOX inhibitor being considered as a treatment for osteoarthritis.

Product Name: Licofelone |Catalog Number: DC8751 |CAS 156897-06-2 |Other names: ML-3000; |Chemical Name:  |Molecule Formular: C23H22ClNO2 |MW: 379.88

Licofelone is a dual COX/LOX inhibitor being considered as a treatment for osteoarthritis.

For research only, not for human use!

Oligomycin A|cas 14104-19-9|DC Chemicals

Oligomycin A|cas 14104-19-9|DC Chemicals

Oligomycin A is an inhibitor of ATP synthase, inhibits oxidative phosphorylation and all the ATP-dependent processes occurring on the coupling membrane of mitochondria.

Product Name: Oligomycin A |Catalog Number: DC8750 |CAS 14104-19-9 |Other names:  |Chemical Name:  |Molecule Formular: C45H74O11 |MW: 791.06

Oligomycin A is an inhibitor of ATP synthase, inhibits oxidative phosphorylation and all the ATP-dependent processes occurring on the coupling membrane of mitochondria.

For research only, not for human use!

Plinabulin|cas 714272-27-2|DC Chemicals

Plinabulin|cas 714272-27-2|DC Chemicals

Plinabulin (NPI-2358) is a vascular disrupting agents (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells.

Product Name: Plinabulin |Catalog Number: DC8749 |CAS 714272-27-2 |Other names: NPI-2358;  NPI 2358 |Chemical Name:  |Molecule Formular: C19H20N4O2 |MW: 336.39

Plinabulin (NPI-2358) is a vascular disrupting agents (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells.in vitro: NPI-2358 binds to the colchicine-binding site of tubulin and has potent inhibitory to human tumor cell lines which have overexpressed Pgp or reduced nuclear Topo II catalytic activity, with IC50 from 9.8 to 18 nM. NPI-2358 is able to rapidly induce tubulin depolymerization in HUVECs and monolayer permeability even at 20 nM. NPI-2358 induces cell death in MM cells with IC50 of 8-10 nM, which due to trigger early mitotic arrest in MM cells. NPI-2358 also inhibits tubule formation and migration of endothelial as well as MM cells, which leads to disrupt tumor vasculature. NPI-2358 could induces cell death in patient MM (CD138+) cells without effecting viability of normal mononuclear cells. Blockade of JNK abrogates NPI-2358-induced mitotic arrest or MM cell death.
in vivo: NPI-2358 (7.5 mg/kg) inhibits tumor growth in human plasmacytoma mouse xenograft models at well-tolerated doses. NPI-2358 induces a time- and dose-dependent decrease in tumour perfusion. NPI-2358 is more sensitive to the KHT sarcoma than the C3H tumour, while radiation response could enhance the antitumor activity in both models.

For research only, not for human use!



MK8745|cas 885325-71-3|DC Chemicals

MK8745|cas 885325-71-3|DC Chemicals

MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B.

Product Name: MK8745 |Catalog Number: DC8748 |CAS 885325-71-3 |Other names:  |Chemical Name:  |Molecule Formular: C20H19ClFN5OS |MW: 431.91

MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B.

For research only, not for human use!

PD-151746|cas 179461-52-0|DC Chemicals

PD-151746|cas 179461-52-0|DC Chemicals

PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain. 

Product Name: PD-151746 |Catalog Number: DC8747 |CAS 179461-52-0 |Other names:  3-(5-Fluoro-3-indolyl)-2-mercapto-(Z)-2-propenoic Acid; AC1NS4NH; SCHEMBL2322924; SCHEMBL2322928; |Chemical Name:  |Molecule Formular: C11H8FNO2S |MW: 237.25

PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain. 

For research only, not for human use!

NSC319726|cas 71555-25-4|DC Chemicals

NSC319726|cas 71555-25-4|DC Chemicals

NSC319726 is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.

Product Name: NSC319726 |Catalog Number: DC8746 |CAS 71555-25-4 |Other names: NSC-319726 |Chemical Name:  |Molecule Formular: C11H14N4S |MW: 234.32

NSC319726 is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.in vitro: For NSC319726, the effect was even greater as the IC50
for the 175 mutant was 8 nM while the IC50 of the WT was not reached. NSC319726 did not induce WT p53 protein levels or transcriptional activity as common cytotoxic agents such as etoposide do in vitro. NSC319726 exhibited a much higher sensitivity for the MEF-p53R172H/R172H cell line as compared to the p53+/+ and p53-/- controls. NSC319726 treatment of a MEF cell line derived from p53R172H/R172H mice resulted in a loss of PAB240 immunoflouresence staining.
in vivo: At a dose of 1mg/kg, tumor growth of the H460 (p53+/+) and MDAMB468 (p53R273W) xenografts was not inhibited relative to the vehicle control whereas tumor growth was significantly inhibited in the TOV112D (p53R175H) xenografts. When we lowered the dose ten-fold to 0.1 mg/kg in the TOV112D mice, we observed only a small difference in tumor growth inhibition demonstrating both a dosage effect of the drug and a larger therapeutic window.Taken together, these findings provide in vivo evidence for allele specific p53 mutant reactivation.

For research only, not for human use!


PU-H71|cas 873436-91-0|DC Chemicals

PU-H71|cas 873436-91-0|DC Chemicals

PU-H71 is a potent Hsp90 inhibitor with IC50 of 50 nM.

Product Name: PU-H71 |Catalog Number: DC8745 |CAS 873436-91-0 |Other names: PU-H 71;  PU H71 |Chemical Name:  |Molecule Formular: C18H21IN6O2S |MW: 512.37

PU-H71 is a potent Hsp90 inhibitor with IC50 of 50 nM.PU-H71, a novel HSP90 inhibitor in Ewing sarcoma cell lines, Hsp90 plays a critical role in modulating the activity of many cell signaling proteins and are an attractive target for anti-cancer therapeutics. Studies indicate that PU-H71(Hsp90 inhibitors) may serve as potential anti-Parkinson′s disease. PU-H71. Potent and durable anti-tumor effects in TNBC xenografts, including complete response and tumor regression, without toxicity to the host are achieved with this agent. Notably, TNBC tumors respond to retreatment with PU-H71 for several cycles extending for over 5 months without evidence of resistance or toxicity.

For research only, not for human use!

PD318088|cas 391210-00-7|DC Chemicals

PD318088|cas 391210-00-7|DC Chemicals

PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

Product Name: PD318088 |Catalog Number: DC8744 |CAS 391210-00-7 |Other names: PD 318088; PD-318088 |Chemical Name:  |Molecule Formular: C16H13BrF3IN2O4 |MW: 561.09

PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.in vitro: PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure.

For research only, not for human use!

NVP-BVU972|cas 1185763-69-2|DC Chemicals

NVP-BVU972|cas 1185763-69-2|DC Chemicals

NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.

Product Name: NVP-BVU972 |Catalog Number: DC8743 |CAS 1185763-69-2 |Other names: NVP-BVU 972 |Chemical Name:  |Molecule Formular: C20H16N6 |MW: 340.38

NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.NVP-BVU972 potently inhibits MET kinase but displays low inhibition against other kinases including the most closely related kinase RON with IC50 values of more than 1000 nM. NVP-BVU972 also suppresses constitutive MET phosphorylation in GTL-16 cells or HGF-stimulated MET phosphorylation in A549 cells with IC50 values of 7.3 nM and 22 nM, respectively. NVP-BVU972 potently prevents the growth of the MET gene amplified cell lines GTL-16, MKN-45 and EBC-1 with IC50 values of 66 nM, 82 nM and 32 nM, respectively. In line with their high frequency in the NVP-BVU972 screen, Y1230 and D1228 mutations give rise to dramatic shifts in the measured IC50 values for NVP-BVU972 in BaF3 cell line. Resistance triggered by V1155L is more limited to NVP-BVU972. A dose-dependent reduction in TPR-MET phosphorylation when applying NVP-BVU972 to BaF3 cells expressing wild-type TPR-MET. Both Y1230H and D1228A mutations abrogated the effect of NVP-BVU972 but not AMG 458. However, F1200I and L1195V interferes with the potency of NVP-BVU972 to prevent TPR-MET phosphorylation.

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PP121|cas 1092788-83-4|DC Chemicals

PP121|cas 1092788-83-4|DC Chemicals

PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.

Product Name: PP121 |Catalog Number: DC8742 |CAS 1092788-83-4 |Other names: PP 121; PP-121 |Chemical Name:  |Molecule Formular: C17H17N7 |MW: 319.36

PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.PP-121 selectivity interacts within a hydrophobic pocket that is conserved between both tyrosine kinases and PI3Ks, not serine-threonine kinases. PP-121 makes a hydrogen bond to Glu310 in Src, effectively substituting for the structural role of the catalytic lysine and resulting in the ordering of helix C and stabilization of an active conformation. PP-121 also inhibits other PI3Ks including p110α and DNA-PK with IC50 of 52 nM and 60 nM, respectively. PP-121 potently and dose-dependently blocks the phosphorylation of Akt, p70S6K and S6 in two glioblastoma cell lines, U87 and LN229. PP-121 potently inhibits the proliferation of a subset of the tumor cell lines by direct inhibition of PI3Ks and mTOR. PP-121 induces a G0/G1 arrest in LN220, U87 and Seg1 cells. PP-121 also blocks tyrosine phosphorylation induced by v-Src in NIH3T3 cells transformed with v-Src(Thr338). PP-121 could restore actin stress fiber staining in NIH3T3 cells transformed with v-Src(Thr338). PP-121 at a low concentration of 40 nM inhibits Ret autophosphorylation in TT thyroid carcinoma cells that express the C634W oncogenic Ret mutant35. PP-121 inhibits cell proliferation with IC50 of 50 nM in TT thyroid carcinoma cells. PP-121 inhibits cell proliferating stimulated only with VEGF with IC50 of 41 nM in human umbilical vein endothelial cells (HUVECs). PP-121 directly inhibits Bcr-Abl induced tyrosine phosphorylation, resulting in drug-induced apoptosis in K562 cells and a combination of apoptosis and cell cycle arrest in Bcr-Abl expressing BaF3 cells.

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Plerixafor octahydrochloride|cas 155148-31-5|DC Chemicals

Plerixafor octahydrochloride|cas 155148-31-5|DC Chemicals

Plerixafor octahydrochloride(AMD3100 8HCL) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

Product Name: Plerixafor octahydrochloride |Catalog Number: DC8741 |CAS 155148-31-5 |Other names: AMD3100 octahydrochloride; JM3100 octahydrochloride; SID791 octahydrochloride |Chemical Name:  |Molecule Formular: C28H62Cl8N8 |MW: 794.47

Plerixafor octahydrochloride(AMD3100 8HCL) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.in vitro: Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF–CEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7.
in vivo: A single topical application of Plerixafor promotes wound healing in diabetic mice by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing the activity of fibroblasts and monocytes/macrophages, thereby increasing both angiogenesis and vasculogenesis. Cohorts of mice are administered with PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor on the 5th day. The number and size of the colonies are highest in IGF1 plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated groups, in combination with Plerixafor.

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SL327|cas 305350-87-2|DC Chemicals

SL327|cas 305350-87-2|DC Chemicals

SL-327 is a cell-permeable vinylogous cyanamide that acts as a selective inhibitor of MEK-1 and MEK-2 (IC50 = 0.18 and 0.22 μM respectively).

Product Name: SL327 |Catalog Number: DC8740 |CAS 305350-87-2 |Other names: SL 327;  SL-327 |Chemical Name:  |Molecule Formular: C16H12F3N3S |MW: 335.35

SL-327 is a cell-permeable vinylogous cyanamide that acts as a selective inhibitor of MEK-1 and MEK-2 (IC50 = 0.18 and 0.22 μM respectively).SL-327 has been shown to block hippocampal LTP via inhibition of the MAPK/ERK cascade, which prevents CREB and Elk-1 phosphorylation, and LTP-dependent gene induction, resulting in rapidly decaying LTP, while being uncompetitive with respect to ATP. Brain penetrant in vivo, blocking fear conditioning and learning in rats, and producing neuroprotection in mice, following systemic administration. SL-327 has also been shown to inhibit ERK1, MEK-3/p38, MEK-4, JNK, and PKC activities when used at higher concentrations.

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Talabostat mesylate|cas 150080-09-4|DC Chemicals

Talabostat mesylate|cas 150080-09-4|DC Chemicals

Talabostat mesilate(PT-100; Val-boroPro) is an orally active, specific inhibitor of dipeptidyl peptidases(IC50=1 nM for DPP4), including tumor-associated fibroblast activation protein.

Product Name: Talabostat mesylate |Catalog Number: DC8739 |CAS 150080-09-4 |Other names: PT-100; ValboroPro; Val-boroPro; PT100; PT 100 |Chemical Name:  |Molecule Formular: C10H23BN2O6S |MW: 310.18

Talabostat mesilate(PT-100; Val-boroPro) is an orally active, specific inhibitor of dipeptidyl peptidases(IC50=1 nM for DPP4), including tumor-associated fibroblast activation protein.By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, talabostat inhibits dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell- dependent activity. This agent may also stimulate the production of colony stimulating factors, such as granulocyte colony stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis. Dipeptidyl peptidases are involved in the activation of polypeptide hormones and chemokines.

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Sal003|cas 1164470-53-4|DC Chemicals

Sal003|cas 1164470-53-4|DC Chemicals

Sal003 is a potent cell-permeable analog of the eIF2α phosphatase inhibitor Salubrinal with enhanced aqueous solubility.

Product Name: Sal003 |Catalog Number: DC8738 |CAS 1164470-53-4 |Other names: Sal-003 |Chemical Name:  |Molecule Formular: C18H15Cl4N3OS |MW: 463.21

Sal003 is a potent cell-permeable analog of the eIF2α phosphatase inhibitor Salubrinal with enhanced aqueous solubility.Sal003 has been shown to prevent dephosphorylation of eIF-2α which has been shown to regulate the late phase of long-term potentiation (LTP) and memory (LTM). This enhanced phosphorylated state of eIF-2α is shown to prevent L-LTP and suppress memory in mice.

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SCH900776 S-isomer|cas 891494-64-|DC Chemicals

SCH900776 S-isomer|cas 891494-64-|DC Chemicals

SCH900776 (S-isomer) is the S-isomer form of SCH900776(HY-15532), which is a potent, selective and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50 = 3 nM), highly selective against Chk2 (IC50 = 1500 nM) and cyclin-dependent kinase CDK2 (IC50 = 160 nM).

Product Name: SCH900776 S-isomer |Catalog Number: DC8737 |CAS 891494-64-7 |Other names: SCH 900776 S-isomer; SCH-900776 S-isomer |Chemical Name:  |Molecule Formular: C15H18BrN7 |MW: 376.25

SCH900776 (S-isomer) is the S-isomer form of SCH900776(HY-15532), which is a potent, selective and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50 = 3 nM), highly selective against Chk2 (IC50 = 1500 nM) and cyclin-dependent kinase CDK2 (IC50 = 160 nM).in vitro: SCH 900776 is a less potent inhibitor of Chk2 and CDK2 with IC50 of 1.5 μM and 0.16 μM, respectively. SCH 900776 shows no significant inhibition of cytochrome P450 human liver microsomal isoforms 1A2, 2C9, 2C19, 2D6, and 3A4. SCH 900776 induces a dose-dependent loss of DNA replication capability 24 hours after hydroxyurea exposure. SCH 900776 enhances the γ-H2AX response of hydroxyurea, 5-fluoruracil, and cytarabine. In combination with an antimetabolite, SCH 900776 induces accumulation of γ-H2AX within 2 hours, indicative of replication fork collapse and double stranded DNA breaks. Additionally, SCH 900776 suppresses accumulation of the Chk1 pS296 autophosphorylation in a dose-dependent manner. Exposure of proliferating WS1 cells to SCH 900776 is associated with rapid, dose-dependent accumulation of Chk1 pS345, indicating that cycling populations of normal cells induce Chk1 pS345 following exposure to SCH 900776 as part of a futile cycle, perhaps driven by AT-family kinases and DNA-PK.
in vivo: Administered 30 minutes after gemcitabine, 4 mg/kg SCH 900776 is sufficient to induce the γ-H2AX biomarker while 8 mg/kg leads to enhanced tumor pharmacodynamic and regression responses relative to gemcitabine or SCH 900776 alone. Dose escalation of SCH 900776 (16 mg/kg and 32 mg/kg) induces incremental improvements in tumor response. Importantly, doses of SCH 900776 associate with robust biomarker activation and improved tumor response are not associated with enhanced toxicity of gemcitabine on hematological parameters in BALB/c mice.

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Tasocitinib (CP 690550,CP690550) supplier DC Chemicals

Tasocitinib (CP 690550,CP690550) supplier DC Chemicals

Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3.

Product Name: Tofacitinib |Catalog Number: DC8736 |CAS 477600-75-2 |Other names: CP-690550; Tofacitinib; tasocitinib |Chemical Name: 3-((3R,4R)-4-Methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile |Molecule Formular: C16H20N6O |MW: 312.37

Tofacitinib (trade name Xeljanz,  Formerly tasocitinib, CP-690550) is a drug discovered and developed by Pfizer. It is currently approved  For the treatment of rheumatoid arthritis (RA) in the United States and is being studied  For treatment of psoriasis, inflammatory bowel disease, and other immunological diseases, as well as  For the prevention of organ transplant rejection.For the detailed information of Tofacitinib (CP-690550) Citrate, the solubility of Tofacitinib (CP-690550) Citrate in water, the solubility of Tofacitinib (CP-690550) Citrate in DMSO, the solubility of Tofacitinib (CP-690550) Citrate in PBS buffer, the animal experiment (test) of  Tofacitinib (CP-690550) Citrate, the cell expriment (test) of Tofacitinib (CP-690550) Citrate, the in vivo, in vitro and clinical trial test of Tofacitinib (CP-690550) Citrate, the EC50, IC50,and Affinity of Tofacitinib (CP-690550) Citrate, Please contact DC Chemicals.

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AHU-377(Sacubitril)|DC Chemicals

AHU-377(Sacubitril)|DC Chemicals

AHU-377 is an inhibitor of neprilysin with IC50 value of 5 nM.

Product Name: AHU-377 hemicalcium salt |Catalog Number: DC8735 |CAS 1369773-39-6 |Other names: AHU-377,AHU 377 ,AHU377  |Chemical Name: 4-[[(2S,4R)-5-ethoxy-4-methyl-5-oxo-1-(4-phenylphenyl)pentan-2-yl]amino]-4-oxobutanoic acid |Molecule Formular: C24H28Ca0.5NO5 |MW: 430.52

For research only, not for human use!

AHU-377(Sacubitril)|DC Chemicals

AHU-377(Sacubitril)|DC Chemicals

AHU-377 is an inhibitor of neprilysin with IC50 value of 5 nM.

Product Name: AHU-377(Sacubitril) |Catalog Number: DC8734 |CAS 149709-62-6 |Other names: AHU-377,AHU 377 ,AHU377  |Chemical Name: 4-[[(2S,4R)-5-ethoxy-4-methyl-5-oxo-1-(4-phenylphenyl)pentan-2-yl]amino]-4-oxobutanoic acid |Molecule Formular: C24H29NO5 |MW: 411.49

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R406 (RN-486)|supplier DC Chemicals

R406 (RN-486)|supplier DC Chemicals

R406 is a potent Syk inhibitor with IC50 of 41 nM and also potently inhibits Flt3.

Product Name: R406 |Catalog Number: DC8733 |CAS 841290-81-1 |Other names: R406,R-406 |Chemical Name: 6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one benzenesulfonate |Molecule Formular: C28H29FN6O8S |MW: 628.63

For the detailed information about the solubility of R406 free base in water, the solubility of R406 free base in DMSO, the solubility of R406 free base in PBS buffer, the animal experiment(test) of R406 free base,the in vivo,in vitro and clinical trial test of R406 free base,the cell experiment(test) of R406 free base,the IC50, EC50 and Affinity of R406 free base, please contact DC Chemicals.

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OTSSP167|OTSSP-167,MELK inhibitor|DC Chemicals

OTSSP167|OTSSP-167,MELK inhibitor|DC Chemicals

OTSSP167 is a highly potent MELK inhibitor (IC50 = 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like).

Product Name: OTSSP167 |Catalog Number: DC8732 |CAS 1431697-89-0 |Other names: MELK inhibitor; OTSSP-167; OTSSP 167 |Chemical Name:  |Molecule Formular: C25H28Cl2N4O2 |MW: 487.42

MELK (maternal embryonic leucine zipper kinase) is a novel therapeutic target  For breast cancer and also reported to be highly upregulated in multiple types of human cancer. OTSSP167 is a highly potent MELK inhibitor (IC50 of 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like). MELK inhibitor OTSSP167 should be a promising compound possibly to suppress the growth of tumor-initiating cells and be applied  For treatment of a wide range of human cancer.For the detailed information of OTSSP167 HCl Salt, the solubility of OTSSP167 HCl Salt in water, the solubility of OTSSP167 HCl Salt in DMSO, the solubility of OTSSP167 HCl Salt in PBS buffer, the animal experiment (test) of  OTSSP167 HCl Salt, the cell expriment (test) of OTSSP167 HCl Salt, the in vivo, in vitro and clinical trial test of OTSSP167 HCl Salt, the EC50, IC50,and Affinity of OTSSP167 HCl Salt, Please contact DC Chemicals.

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Lesinurad sodium (RDEA594 sodium)|DC Chemicals

Lesinurad sodium (RDEA594 sodium)|DC Chemicals

Lesinurad sodium (RDEA594 sodium) is an once-daily inhibitor of URAT1; URAT1 is a transporter in the kidney that regulates uric acid excretion from the body.

Product Name: Lesinurad sodium |Catalog Number: DC8731 |CAS 1151516-14-1 |Other names: RDEA-594 sodium |Chemical Name:  |Molecule Formular: C17H13BrN3NaO2S |MW: 426.26

Lesinurad sodium (RDEA594 sodium) is an once-daily inhibitor of URAT1; URAT1 is a transporter in the kidney that regulates uric acid excretion from the body.
IC50 Value:
in vivo: In healthy subjects, the combination of 40 mg FBX with RDEA-594 reduced sUA by approximately 70% at the 200 mg and 400 mg RDEA-594 dose levels, respectively. In gout patients, FBX 40 mg and 80 mg alone reduced sUA by 35% and 47%, respectively. FBX 40 mg + RDEA-594 reduced sUA by 56% and 61% when combined with RDEA-594 400 mg or 600 mg. respectively, resulting in response rates of 100% for sUA <6 and <5 mg/dl and 64% <4 mg/dl. FBX 80 mg + RDEA-594 reduced sUA by 65% and 73% when combined with RDEA-594 400 mg or 600 mg respectively. Following single dosing of RDEA594, exposure of RDEA594 was significantly higher than those obtained from RDEA 806 dosing, >5X at 20 mg/kg in rats and >10X at 30 mg/kg in monkeys.Clinical trial: Lesinurad and Febuxostat Combination Extension Study in Gout .Phase3

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Cambendazol|CAS 26097-80-3|DC Chemicals

Cambendazol|CAS 26097-80-3|DC Chemicals

Product Name: Cambendazol |Catalog Number: DC8730 |CAS 26097-80-3 |Other names: NSC377071;Novazole;MK 905;Noviben;Bonlam |Chemical Name:  |Molecule Formular: C14H14N4O2S |MW: 302.35

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Bifeprunox |CAS 350992-10-8|DC Chemicals

Bifeprunox |CAS 350992-10-8|DC Chemicals

Product Name: Bifeprunox |Catalog Number: DC8729 |CAS 350992-10-8 |Other names:  |Chemical Name:  |Molecule Formular: C24H23N3O2 |MW: 385.46

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CH5424802(Alectinib)|DC Chemicals|Price|Buy|DC Chemicals

CH5424802(Alectinib)|DC Chemicals|Price|Buy|DC Chemicals

CH5424802(AF 802; Alectinib) is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M mutation.

Product Name: CH5424802(Alectinib HCl) |Catalog Number: DC8728 |CAS 1256589-74-8 |Other names: AF-802; CH 5424802; CH-5424802; AF802; AF 802 |Chemical Name: 9-ethyl-6,6-dimethyl-8-(4-morpholinopiperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile |Molecule Formular: C30H37ClN4O2 |MW: 521.1

The dissociation constant (KD) value of CH5424802  For ALK in an ATP-competitive manner is 2.4 nM. CH5424802 has substantial inhibitory potency against both native ALK and L1196M with Ki of 0.83 nM and 1.56 nM, respectively. CH5424802 prevents autophosphorylation of ALK in NCI-H2228 NSCLC cells expressing EML4-ALK. CH5424802 also suppresses the phosphorylation of STAT3 and AKT, but not of ERK1/2. CH5424802 completely inhibits the phosphorylation of STAT3 at Tyr705. CH5424802 is preferentially efficacious against NCI-H2228 cells expressing EML4-ALK, but not ALK fusion-negative NSCLC cell lines, including HCC827 cells (EGFR exon 19 deletion), A549 cells (KRAS mutant), or NCI-H522 cells (EGFR wild-type, KRAS wild-type, and ALK wild-type) in monolayer culture. CH5424802 elicits an apoptotic marker—caspase-3/7-like activation—in NCI-H2228 spheroid cells. CH5424802 blocks the growth of two lymphoma lines, KARPAS-299 and SR, with NPM-ALK fusion protein but does not influence the growth of an HDLM-2 lymphoma line without ALK fusion. [1] CH5424802 displays high target selectivity and the stronger anti-proliferative activity against KARPAS-299. CH5424802 inhibits KAPRAS-299 with an IC50 of 3 nM, and KDR with IC50 of 1.4 μM. The metabolic stability of CH5424802 is very high.[2] Oral administration of CH5424802 dose-dependently inhibits tumor growth with an ED50 of 0.46 mg/kg and tumor regression. Treatment of 20 mg/kg CH5424802 reveals rapid tumor regression by 168%, the tumor volume in any mouse is <30 mm3 after 11 days of treatment (at day 28), a potent antitumor effect is maintained, and tumor regrowth does not occur throughout the 4-week drug-free period. The half-life and the oral bioavailability of CH5424802 in mice are 8.6 hours and 70.8%, respectively. At a repeated dose of 6 mg/kg, the mean plasma levels reached 1.7, 1.5, and 0.3 nM at 2, 7, and 24 hours post-dose, respectively. Administration of CH5424802 leads to tumor growth prevention and tumor regression. Tumor growth inhibition at 20 mg/kg is 119%  For KARPAS-299 and 104%  For NB-1 on day 20. CH5424802 inhibits the phosphorylation of STAT3 in a dose-dependent manner (2–20 mg/kg). A partial decrease in AKT phosphorylation is also observed in CH5424802-treated xenograft tumors. [1]For the detailed information of CH5424802, the solubility of CH5424802 in water, the solubility of CH5424802 in DMSO, the solubility of CH5424802 in PBS buffer, the animal experiment (test) of  CH5424802, the cell expriment (test) of CH5424802, the in vivo, in vitro and clinical trial test of CH5424802, the EC50, IC50,and Affinity of CH5424802, Please contact DC Chemicals.

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PF04880594|cas|DC Chemicals

PF04880594|cas|DC Chemicals

PF-04880594 is an inhibitor of RAF with IC50 values of 0.19 nM/0.13 nM and 0.39 nM for BRAF/BRAFV599E and c-RAF, respectively.

Product Name: PF-04880594 |Catalog Number: DC8727 |CAS 1111636-35-1 |Other names: PF 04880594,PF04880594 |Chemical Name: 3-[[4-[1-(2,2-difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazol-4-yl]pyrimidin-2-yl]amino]propanenitrile |Molecule Formular: C19H16F2N8   |MW: 394.38

PF-04880594 is a potent and selective RAF inhibitor that inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 potently inhibits tumor growth in BRAF-mutant melanoma xenograft models.

For research and scientific purpose only, not for human use!

FLLL31,FLLL-31|cas 52328-97-9|STAT inhibitor|DC Chemicals

FLLL31,FLLL-31|cas 52328-97-9|STAT inhibitor|DC Chemicals

FLLK31 is a potent and selective inhibitor of the STAT3 signaling pathway.

Product Name: FLLL31 |Catalog Number: DC8726 |CAS 52328-97-9 |Other names: FLLL31,FLLL-31,FLLL 31 |Chemical Name: (E,E)-1,7-Bis(3,4-dimethoxyphenyl)-4,4-dimethyl-1,6-heptadiene-3,5-dione Tetramethylcurcumin |Molecule Formular: C25H28O6 |MW: 424.49

FLLL31 selectively binds to Janus kinase 2 and the STAT3 Src homology-2 (SH2) domain, effective inhibitors of STAT3 phosphorylation. STAT3 plays a critical role in early embryogenesis, but is largely dispensable in normal adult cells and tissues. On the other hand the JAK2/STAT3 signaling pathway is persistently activated in great number of human solid and blood cancers. Such activation is commonly associated with a worse prognosis. FLLL31 is a curcumin derivative locked in diketone-tautomeric form, which supposedly improves binding to SH2 domain. The compound inhibits JAK2 kinase activity and prevents STAT3 phosphorylation. FLLK31 is a potent and selective inhibitor of the STAT3 signaling pathway.

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NSC 23766,NSC23766|Rac GTPase inhibitor|DC Chemicals

NSC 23766,NSC23766|Rac GTPase inhibitor|DC Chemicals

NSC 23766 is a specific inhibitor of the binding and activation of Rac GTPase.

Product Name: NSC 23766 |Catalog Number: DC8725 |CAS 1177865-17-6 |Other names: NSC 23766,NSC23766,NSC-23766 |Chemical Name: N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrochloride |Molecule Formular: C24H35N7.3HCl |MW: 530.97

NSC 23766 is a specific inhibitor of the binding and activation of Rac GTPase. In vitro studies have shown that NSC 23766 inhibits Rac 1 binding and activation via Rac-specific GEF Trio or Tiam 1 without altering RhoA or CDC42 binding or activation. Membrane type 1-matrix metalloproteinases (MT-1MMP) expression in CB CD34+ cells has been reported to decrease in the presence of NSC 23766. Silveta compressa investigations indicate that NSC 23766 depolarizes endomembrane cycling, altered polar adhesive secretion, and tip growth.

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