2016年12月29日星期四

Eleclazine(GS-6615)|late sodium current inhibitor

Eleclazine(GS-6615)|late sodium current inhibitor

Eleclazine(GS-6615) is a selective late sodium current inhibitor.

Product Name: Eleclazine(GS-6615)|Cat No: DC9980|cas: 1443211-72-0 |Other Names: GS6615,GS 6615

Eleclazine, also known as GS-6615, is a selective late sodium current inhibitor. Eleclazine is potentially useful for treatment of coronary vasodilators, antiarrhythmics and vasodilators. Eleclazin showed a shortening of the QTc interval (the time interval between the start of the Q-wave and end of the T-wave in the heart’s electrical cycle) in patients with long QT-3 (LQT3) syndrome. LQT3 is a genetic disorder that prolongs the heart’s QTc interval and can cause life-threatening cardiac arrhythmias (abnormal heartbeats).

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

PRX08066,PRX 08066|5-HT2BR antagonist

PRX08066,PRX 08066|5-HT2BR antagonist

PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.

Product Name: PRX-08066|Cat No: DC9979|cas: 866206-54-4|Other Names: PRX08066,PRX 08066

PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
in vitro: PRX-08066 inhibits 5-HT-induced mitogen-activated protein kinase activation with IC50 of 12 nM and markedly reduces thymidine incorporation with IC50 of 3 nM in Chinese hamster ovary cells expressing the human 5-HT2BR, which suggests that PRX-08066 can potentially inhibit the pathologic 5-HT-induced vascular muscularization associated with PAH [1]. PRX-08066 inhibits cell proliferation with IC50 of 0.46 nM and with a maximum inhibition of 20% and 5-HT secretion with IC50 of 6.9 nM with a maximum inhibition of 30% in the 5-HT(2B) expressing SI-NET cell line, KRJ-I. PRX-08066 inhibits isoproterenol-stimulated 5-HT release with IC50 of 1.25 nM and a maximum inhibition of 60% in NCI-H720 cells. PRX-08066 (0.5 nM) significantly inhibits ERK phosphorylation in KRJ-I cells. PRX-08066 inhibits TGFβ1, CTGF and FGF2 transcription and secretion in KRJ-I cells. PRX-08066 decreases level of transcripts for Ki67 (84%) as well as Ki67 protein (36.8%) associated with an increase in caspase 3 transcript levels in KRJ-I cells. PRX-08066 decreases level of transcripts of TGFβ1, FGF2 and TPH1 in KRJ-I cells. PRX-08066 significantly increases the number of dead cells (34%) compared with untreated controls in KRJ-I cells. PRX-08066 causes a significant increase in dead/caspase 3 positive cells (76%) and caspase 3 activity (52%) in HEK293 cells.
in vivo: PRX-08066 (100 mg/kg) treated groups demonstrates less right ventricular hypertrophy and septal flattening than the monocrotaline control group in rats. PRX-08066 significantly reduces peak pulmonary artery pressure at 50 mg/kg and 100 mg/kg compared with monocrotaline control rats. PRX-08066 also significantly reduces right ventricle (RV)/body weight and RV/left ventricle + septum, compared with MCT-treated rats. PRX-08066 significantly attenuates the elevation in pulmonary artery pressure and RV hypertrophy and maintains cardiac function. PRX-08066 significantly reduces the hypoxia-dependent increase in right ventricular systolic pressure in both rats and mice without affecting the systemic mean arterial pressure in the animals. PRX-08066 (100 mg/kg) significantly inhibits both right ventricular systolic pressure and right ventricular/left ventricular +septum weight elevations in rats. PRX-08066 (30 mg/kg) inhibits right ventricular systolic pressure and monocrotaline-induced ERK phosphorylation in whole lung homogenates in rats.

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

4-oxo-4-HPR|4-oxo-4-fenretinide|865536-65-8

4-oxo-4-HPR|4-oxo-4-fenretinide|865536-65-8

4-oxo-4-HPR is a recently identified fenretinide metabolite, induces marked G2-M cell cycle arrest and apoptosis in fenretinide-sensitive and fenretinide-resistant cell lines.

Product Name: 4-oxo-4-HPR|Cat No: DC9978|cas: 865536-65-8|Other Names: 4-oxo-4-fenretinide

4-oxo-4-HPR was two to four times more effective than 4-HPR in most cell lines, was effective in both 4-HPR-sensitive and 4-HPR-resistant cells, and, in combination with 4-HPR, caused a synergistic effect. The tumor growth-inhibitory effects of 4-oxo-4-HPR seem to be independent of nuclear retinoid receptors (RAR), as indicated by the failure of RAR antagonists to inhibit its effects and by its poor ability to bind and transactivate RARs. Unlike 4-HPR, which only slightly affected the G(1) phase of the cell cycle, 4-oxo-4-HPR caused a marked accumulation of cells in G(2)-M. This effect was associated with a reduction in the expression of regulatory proteins of G(2)-M (cyclin-dependent kinase 1 and cdc25c) and S (cyclin A) phases, and with an increase in the expression of apoptosis-related proteins, such as p53 and p21. Apoptosis was induced by 4-oxo-4-HPR in both 4-HPR-sensitive and 4-HPR-resistant cells and involved activation of caspase-3 and caspase-9 but not caspase-8. We also showed that 4-oxo-4-HPR, similarly to 4-HPR, increased reactive oxygen species generation and ceramide levels by de novo synthesis. In conclusion, 4-oxo-4-HPR is an effective 4-HPR metabolite that might act as therapeutic agent per se and, when combined with 4-HPR, might improve 4-HPR activity or overcome 4-HPR resistance.

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

VU0155041||VU0155041|mGlu4 modulator

VU0155041||VU0155041|mGlu4 modulator

VU0155041 is a Potent, positive allosteric modulator/allosteric agonist at mGlu4 receptors (EC50 = 798 and 693 nM at human and rat mGlu4 receptors respectively).

Product Name: VU0155041|Cat No: DC9977|cas: 1093757-42-6|Other Names: VU0155041,VU-0155041

Potent, positive allosteric modulator/allosteric agonist at mGlu4 receptors (EC50 = 798 and 693 nM at human and rat mGlu4 receptors respectively). Active in in vivo models of Parkinson's disease following i.c.v. administration.

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

(+)-Narwedin||D-Narwedin|CAS 7318-5-0

(+)-Narwedin||D-Narwedin|CAS 7318-5-0

(+)-Narwedin. Galantamine(Narwedin) is a competitive and reversible cholinesterase(AChE) inhibitor.

Product Name: (+)-Narwedin|Cat No: DC9976|cas: 7318-5-0|Other Names: D-Narwedin,(+)Narwedin,+Narwedin

LY2365109 is a potent and selective GlyT1 inhibitors with IC50 value of 15.8 nM.

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

LY2365109||LY-2365109| GlyT1 inhibitor

LY2365109||LY-2365109| GlyT1 inhibitor

LY2365109 is a potent and selective GlyT1 inhibitors with IC50 value of 15.8 nM.

Product Name: LY2365109|Cat No: DC9975|cas: 868265-28-5|Other Names: LY 2365109,LY-2365109

LY2365109 is a potent and selective GlyT1 inhibitors with IC50 value of 15.8 nM.

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

Osilodrostat(LCI699)||aldosterone synthase/aromatase inhibitor

Osilodrostat(LCI699)||aldosterone synthase/aromatase inhibitor

Osilodrostat is an inhibitor of aldosterone synthase and aromatase, for treating Cushing’s disease.

Product Name: Osilodrostat(LCI699) free base|Cat No: DC9974|cas: 928134-65-0|Other Names: LCI 699,LCI-699

Osilodrostat, as modulators of 11-β-hydroxylase, useful for treating a disorder ameliorated 11-β-hydroxylase inhibition eg Cushing’s disease, hypertension, congestive heart failure, metabolic syndrome, liver diseases, cerebrovascular diseases, migraine headaches, osteoporosis or prostate cancer.Novartis is developing osilodrostat, an inhibitor of aldosterone synthase and aromatase, for treating Cushing’s disease. In July 2016, osilodrostat was reported to be in phase 3 clinical development.The somatostatin analog pasireotide and the 11β-hydroxylase inhibitor osilodrostat (LCI699) reduce cortisol levels by distinct mechanisms of action. There exists a scientific rationale to investigate the clinical efficacy of these two agents in combination. This manuscript reports the results of a toxicology study in rats, evaluating different doses of osilodrostat and pasireotide alone and in combination. Sixty male and 60 female rats were randomized into single-sex groups to receive daily doses of pasireotide (0.3mg/kg/day, subcutaneously), osilodrostat (20mg/kg/day, orally), osilodrostat/pasireotide in combination (low dose, 1.5/0.03mg/kg/day; mid-dose, 5/0.1mg/kg/day; or high dose, 20/0.3mg/kg/day), or vehicle for 13weeks. Mean body-weight gains from baseline to Week 13 were significantly lower in the pasireotide-alone and combined-treatment groups compared to controls, and were significantly higher in female rats receiving osilodrostat monotherapy. Osilodrostat and pasireotide monotherapies were associated with significant changes in the histology and mean weights of the pituitary and adrenal glands, liver, and ovary/oviduct. Osilodrostat alone was associated with adrenocortical hypertrophy and hepatocellular hypertrophy. In combination, osilodrostat/pasireotide did not exacerbate any target organ changes and ameliorated the liver and adrenal gland changes observed with monotherapy. Cmax and AUC0-24h of osilodrostat and pasireotide increased in an approximately dose-proportional manner. In conclusion, the pasireotide and osilodrostat combination did not exacerbate changes in target organ weight or toxicity compared with either monotherapy, and had an acceptable safety profile; addition of pasireotide to the osilodrostat regimen may attenuate potential adrenal gland hyperactivation and hepatocellular hypertrophy, which are potential side effects of osilodrostat monotherapy.The somatostatin analog pasireotide and the 11β-hydroxylase inhibitor osilodrostat (LCI699) reduce cortisol levels by distinct mechanisms of action. There exists a scientific rationale to investigate the clinical efficacy of these two agents in combination. This manuscript reports the results of a toxicology study in rats, evaluating different doses of osilodrostat and pasireotide alone and in combination. Sixty male and 60 female rats were randomized into single-sex groups to receive daily doses of pasireotide (0.3 mg/kg/day, subcutaneously), osilodrostat (20 mg/kg/day, orally), osilodrostat/pasireotide in combination (low dose, 1.5/0.03 mg/kg/day; mid-dose, 5/0.1 mg/kg/day; or high dose, 20/0.3 mg/kg/day), or vehicle for 13 weeks. Mean body-weight gains from baseline to Week 13 were significantly lower in the pasireotide-alone and combined-treatment groups compared to controls, and were significantly higher in female rats receiving osilodrostat monotherapy. Osilodrostat and pasireotide monotherapies were associated with significant changes in the histology and mean weights of the pituitary and adrenal glands, liver, and ovary/oviduct. Osilodrostat alone was associated with adrenocortical hypertrophy and hepatocellular hypertrophy. In combination, osilodrostat/pasireotide did not exacerbate any target organ changes and ameliorated the liver and adrenal gland changes observed with monotherapy. Cmax and AUC0–24h of osilodrostat and pasireotide increased in an approximately dose-proportional manner.

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

Osilodrostat(LCI699)||aldosterone synthase/aromatase inhibitor

Osilodrostat(LCI699)||aldosterone synthase/aromatase inhibitor

Osilodrostat is an inhibitor of aldosterone synthase and aromatase, for treating Cushing’s disease.

Product Name: Osilodrostat(LCI699) phosphate|Cat No: DC9973|cas: 1315449-72-9|Other Names: LCI 699,LCI-699

Osilodrostat, as modulators of 11-β-hydroxylase, useful for treating a disorder ameliorated 11-β-hydroxylase inhibition eg Cushing’s disease, hypertension, congestive heart failure, metabolic syndrome, liver diseases, cerebrovascular diseases, migraine headaches, osteoporosis or prostate cancer.Novartis is developing osilodrostat, an inhibitor of aldosterone synthase and aromatase, for treating Cushing’s disease. In July 2016, osilodrostat was reported to be in phase 3 clinical development.The somatostatin analog pasireotide and the 11β-hydroxylase inhibitor osilodrostat (LCI699) reduce cortisol levels by distinct mechanisms of action. There exists a scientific rationale to investigate the clinical efficacy of these two agents in combination. This manuscript reports the results of a toxicology study in rats, evaluating different doses of osilodrostat and pasireotide alone and in combination. Sixty male and 60 female rats were randomized into single-sex groups to receive daily doses of pasireotide (0.3mg/kg/day, subcutaneously), osilodrostat (20mg/kg/day, orally), osilodrostat/pasireotide in combination (low dose, 1.5/0.03mg/kg/day; mid-dose, 5/0.1mg/kg/day; or high dose, 20/0.3mg/kg/day), or vehicle for 13weeks. Mean body-weight gains from baseline to Week 13 were significantly lower in the pasireotide-alone and combined-treatment groups compared to controls, and were significantly higher in female rats receiving osilodrostat monotherapy. Osilodrostat and pasireotide monotherapies were associated with significant changes in the histology and mean weights of the pituitary and adrenal glands, liver, and ovary/oviduct. Osilodrostat alone was associated with adrenocortical hypertrophy and hepatocellular hypertrophy. In combination, osilodrostat/pasireotide did not exacerbate any target organ changes and ameliorated the liver and adrenal gland changes observed with monotherapy. Cmax and AUC0-24h of osilodrostat and pasireotide increased in an approximately dose-proportional manner. In conclusion, the pasireotide and osilodrostat combination did not exacerbate changes in target organ weight or toxicity compared with either monotherapy, and had an acceptable safety profile; addition of pasireotide to the osilodrostat regimen may attenuate potential adrenal gland hyperactivation and hepatocellular hypertrophy, which are potential side effects of osilodrostat monotherapy.The somatostatin analog pasireotide and the 11β-hydroxylase inhibitor osilodrostat (LCI699) reduce cortisol levels by distinct mechanisms of action. There exists a scientific rationale to investigate the clinical efficacy of these two agents in combination. This manuscript reports the results of a toxicology study in rats, evaluating different doses of osilodrostat and pasireotide alone and in combination. Sixty male and 60 female rats were randomized into single-sex groups to receive daily doses of pasireotide (0.3 mg/kg/day, subcutaneously), osilodrostat (20 mg/kg/day, orally), osilodrostat/pasireotide in combination (low dose, 1.5/0.03 mg/kg/day; mid-dose, 5/0.1 mg/kg/day; or high dose, 20/0.3 mg/kg/day), or vehicle for 13 weeks. Mean body-weight gains from baseline to Week 13 were significantly lower in the pasireotide-alone and combined-treatment groups compared to controls, and were significantly higher in female rats receiving osilodrostat monotherapy. Osilodrostat and pasireotide monotherapies were associated with significant changes in the histology and mean weights of the pituitary and adrenal glands, liver, and ovary/oviduct. Osilodrostat alone was associated with adrenocortical hypertrophy and hepatocellular hypertrophy. In combination, osilodrostat/pasireotide did not exacerbate any target organ changes and ameliorated the liver and adrenal gland changes observed with monotherapy. Cmax and AUC0–24h of osilodrostat and pasireotide increased in an approximately dose-proportional manner.

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

ARQ-092|ARQ092|AKT inhibitor

ARQ-092|ARQ092|AKT inhibitor

ARQ 092 is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3).

Product Name: ARQ-092|Cat No: DC9972|cas: 1313881-70-7|Other Names: ARQ092,ARQ 092

ARQ 092 is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3). ARQ 092 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may lead to the reduction in tumor cell proliferation and the induction of tumor cell apoptosis. ARQ-092 demonstrated high enzymatic potency against AKT1, AKT2, and AKT3, as well as potent cellular inhibition of AKT activation and the phosphorylation of the downstream target PRAS40. ARQ-092 also served as a potent inhibitor of the AKT1-E17K mutant protein and inhibited tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.

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


IDE-2|IDE2|ESCs inducer

IDE-2|IDE2|ESCs inducer

IDE-2 is a cell-permeable inducer of definitive endoderm formation in mouse and human embryonic stem cells (ESCs) (EC50 = 223 nM for induction of Sox17 expression in ESCs).

Product Name: IDE-2|Cat No: DC9971|cas: 1136466-93-7|Other Names: IDE-2,IDE 2,IDE2

IDE-2 is a cell-permeable inducer of definitive endoderm formation in mouse and human embryonic stem cells (ESCs) (EC50 = 223 nM for induction of Sox17 expression in ESCs). Reported to activate TGF-β signaling and downstream Smad2 phosphorylation; upregulates Nodal expression. Promotes pancreatic progenitor cell formation in vitro, and gut tube formation in vivo.

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

IDE-1|IDE1|ESCs inducer

IDE-1|IDE1|ESCs inducer

IDE-1 induces definitive endoderm formation in mouse and human embryonic stem cells (ESCs) (EC50 = 125 nM).

Product Name: IDE-1|Cat No: DC9970|cas: 1160927-48-9|Other Names: IDE-1,IDE1,IDE 1

IDE-1 induces definitive endoderm formation in mouse and human embryonic stem cells (ESCs) (EC50 = 125 nM). Thought to activate the TGF-β signaling pathway; induces Smad2 phosphorylation and increases levels of Nodal expression.


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

CCT251921|CCT-251921|CDK8/CDK19 inhibitor

CCT251921|CCT-251921|CDK8/CDK19 inhibitor

CCT251921 is a potent, selective, and orally bioavailable small-molecule modulators of the mediator complex-associated kinases CDK8 and CDK19. (IC50 data: CDK8:=2.3 nM; CDK19 = 2.6 nM).

Product Name: CCT251921|Cat No: DC9969|cas: 1607837-31-9|Other Names: CCT-251921,CCT 251921

CCT251921 is a potent, selective, and orally bioavailable small-molecule modulators of the mediator complex-associated kinases CDK8 and CDK19. (IC50 data: CDK8:=2.3 nM; CDK19 = 2.6 nM). CCT251921 showed the optimal compromise of in vitro biochemical, pharmacokinetic, and physicochemical properties and is suitable for progression to animal models of cancer. The Mediator complex-associated cyclin-dependent kinase CDK8 has been implicated in human disease, particularly in colorectal cancer where it has been reported as a putative oncogene.

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

CCT251545|CCT-251545|WNT inhibitor

CCT251545|CCT-251545|WNT inhibitor

CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.

Product Name: CCT251545|Cat No: DC9968|cas: 1661839-45-7|Other Names: CCT-251545,CCT 251545

CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.
in vitro: CCT251545 is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases. CCT251545 also reduces phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM. CCT251545 is a small-molecule inhibitor of the WNT pathway discovered through cell-based screening. CCT251545 displays potent cell-based activity. CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1. CCT251545 demonstrates weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0 ± 0 μM). CCT251545 potently inhibits reporter-based readouts of basal WNT pathway activity in LS174T and SW480 cells in the absence of WNT ligand or other stimulants (IC50 = 0.023 ± 0.011 μM and 0.190 ± 0.030 μM, respectively) and demonstrated potent inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC50 = 0.007 μM)
in vivo: CCT251545 as a potent and selective chemical probe suitable for cell-based exploration of the reported context-dependent roles of CDK8 and CDK19 and associated kinase module subunits in human disease and other biological settings.

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

SQ22536|SQ 22536|adenylyl cyclase inhibitor

SQ22536|SQ 22536|adenylyl cyclase inhibitor

SQ 22536 is a inhibitor of adenylyl cyclase (IC50 = 1.4 μM).

Product Name: SQ22536|Cat No: DC9967|cas: 17318-31-9|Other Names: SQ 22536,SQ-22536

SQ 22536 is a inhibitor of adenylyl cyclase (IC50 = 1.4 μM). Inhibits PGE1-stimulated increases in cAMP levels in intact human platelets.

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

MK-1064|MK1064|2-SORA antagonist

MK-1064|MK1064|2-SORA antagonist

MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia.

Product Name: MK-1064|Cat No: DC9966|cas: 1207253-08-4|Other Names: MK1064,MK 1064

MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia. MK-1064 promotes sleep and increases both rapid eye movement (REM) and non-REM (NREM) sleep in rats at OX2R occupancies higher than the range observed for dual orexin receptor antagonists. MK-1064 increases NREM and REM sleep in dogs without inducing cataplexy. The reference for animal administration is 30 mg/kg.

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

UNC3866|UNC-3866|CBX4/CBX7 chromodomains antagonist

UNC3866|UNC-3866|CBX4/CBX7 chromodomains antagonist

UNC3866 is a potent and selective antagonist of CBX4 and CBX7 chromodomains with (Kd ≈ 100 nM). It is 6- to 63-fold selective for these chromodomains over the other CBX and CDY chromodomains.

Product Name: UNC3866|Cat No: DC9965|cas: 1872382-47-2|Other Names: UNC 3866,UNC-3866

UNC3866 is a potent and selective antagonist of CBX4 and CBX7 chromodomains with (Kd ≈ 100 nM). It is 6- to 63-fold selective for these chromodomains over the other CBX and CDY chromodomains. UNC3866 was also highly selective versus >250 other molecular targets including chromatin regulatory proteins and a general pharmacology panel. UNC3866 was enabled in part by the use of molecular dynamics simulations performed with CBX7 and its endogenous substrate.

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

BEC|inhibitor of arginases I and II

BEC|inhibitor of arginases I and II

BEC is a boronic acid-based arginine analog that acts as a slow-binding, competitive transition state inhibitor of arginase I and II (Ki = 310 nM for human recombinant type II arginase, pH 7.5).

Product Name: BEC hydrochloride|Cat No: DC9964|cas: 222638-67-7|Other Names:

BEC, Hydrochloride is a boronic acid-based arginine analog that acts as a slow-binding, competitive transition state inhibitor of arginase I and II (Ki = 310 nM for human recombinant type II arginase, pH 7.5). BEC does not inhibit nitric oxide synthase (NOS), it causes significant enhancement of NO-dependent smooth muscle relaxation in human penile corpus cavernosum tissue.

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

KRIBB-11|KRIBB11|HSF inhibitor

KRIBB-11|KRIBB11|HSF inhibitor

KRIBB11 is a Heat shock factor (HSF) inhibitor (IC50 = 1.2 μM).

Product Name: KRIBB11|Cat No: DC9963|cas: 342639-96-7|Other Names: KRIBB 11,KRIBB-11

Heat shock factor (HSF) inhibitor (IC50 = 1.2 μM). Increases apoptosis in cancer cells treated with the HSP90 inhibitors Geldanamycin and 17-AAG. Blocks downstream induction of HSP27 and HSP70. Inhibits tumor growth in vivo.

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

YM-58483||CRAC channels/subsequent Ca2+ inhibitor

YM-58483||CRAC channels/subsequent Ca2+ inhibitor

YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.

Product Name: YM-58483|Cat No: DC9962|cas: 223499-30-7|Other Names: YM58483; YM 58483; BPT2

YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.In Vitro: YM-58483 can decrease the levels of P-ERK and P-CREB, without affecting the expression of CD11b and GFAP. YM-58483 also inhibits the release of spinal cord IL-1β, TNF-α, and PGE2[1]. YM-58483 and cyclosporine A inhibits T cell proliferation in a one-way mixed lymphocyte reaction (mLR) with IC50 values of 330 and 12.7 nM, respectively[2]. YM-58483 inhibits DNP antigen-induced histamine release from and leukotrienes (LTs) production in IgE-primed RBL-2H3 cells, a rat basophilic leukemia cell line, with IC50 values of 460 and 310 nM, respectively. YM-58483 also inhibits phytohemagglutinin-P (PHA)-stimulated IL-5 and IL-13 production in human peripheral blood cells with IC50 values of 125 and 148 nM, respectively, which is approximately 5 times less potent than prednisolone. YM-58483 inhibits IL-4 and IL-5 production in a conalbumine-stimulated murine Th2 T cell clone (D10.G4.1), and IL-5 production in phytohemagglutinin-stimulated human whole blood cells with IC50 values comparable to those reported for its CRAC channel inhibition (around 100 nM).
In Vivo: Intrathecal YM-58483 at the concentration of 300 μM (1.5 nmol) and 1000 μM (10 nmol) produces a significant central analgesic effect on the SNL rats[1]. In the mouse graft-versus-host disease (GVHD) model, YM-58483 (1-30 mg/kg, p.o.) and cyclosporine A (1-30 mg/kg, p.o.) inhibit donor anti-host cytotoxic T lymphocyte (CTL) activity and IFN-γ production, and also reduce the number of donor T cells, especially donor CD8+ T cells, in the spleen. YM-58483 (1-10 mg/kg, p.o.) and cyclosporine A (2, 10 mg/kg, p.o.) inhibit the sheep red blood cell (SRBC)-induced delayed type hypersensitivity (DTH) response[2]. M-58483 (30 mg/kg, p.o.) significantly suppresses ovalbumin (OVA)-induced bronchoconstriction in OVA-sensitized guinea pigs, whereas prednisolone does not. YM-58483 (3-30 mg/kg, p.o.) and prednisolone (100 mg/kg, p.o.) both significantly and completely suppress airway hyperresponsiveness (AHR) caused by OVA exposure. YM-58483 inhibits antigen-induced eosinophil infiltration into airways, and decreases IL-4 and cysteinyl-leukotrienes content in inflammatory airways induced in actively sensitized Brown Norway rats. Orally administered YM-58483 prevents antigen-induced late phase asthmatic broncoconstriction and eosinophil infiltration in actively sensitized guinea pigs.

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

STO-609|STO609|Ca2+-calmodulin-dependent protein inhibitor

STO-609|STO609|Ca2+-calmodulin-dependent protein  inhibitor

STO-609 acetate is a selective, cell-permeable inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki values are 80 and 15 ng/ml for inhibition of CaM-KKα and CaM-KKβ respectively); competes for the ATP-binding site.

Product Name: STO-609 acetate  |Cat No: DC9961|cas: 1173022-21-3|Other Names: STO609,STO 609

Selective, cell-permeable inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki values are 80 and 15 ng/ml for inhibition of CaM-KKα and CaM-KKβ respectively); competes for the ATP-binding site. Displays > 80-fold selectivity over CaMK1, CaMK2, CaMK4, MLCK, PKC, PKA and p42 MAPK.

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

HTHQ|anti-oxidative agent

HTHQ|anti-oxidative agent

HTHQ, which is a hydroquinone monoalkyl ether, is a potent anti-oxidative agent, even at low dose levels.

Product Name: HTHQ|Cat No: DC9960|cas: 148081-72-5|Other Names:

HTHQ, which is a hydroquinone monoalkyl ether, is a potent anti-oxidative agent, even at low dose levels.

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

Endoxifen (E-isomer)|SERM|cas 1197194-61-8

Endoxifen (E-isomer)|SERM|cas 1197194-61-8

Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).

Product Name: Endoxifen (E-isomer)|Cat No: DC9959|cas: 1197194-61-8|Other Names: E-Endoxifen

Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).Endoxifen is considered a prodrug, since it has a much higher potency for the estrogen receptor than its parent drug. Endoxifen inhibits the hERG channel protein trafficking to the plasma membrane in a concentration-dependent manner with Endoxifen being more potent than Tamoxifen.Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen observed in Tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher Endoxifen concentrations are needed when ERβ is absent.

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

U 93631|U93631|GABAA receptor ligand

U 93631|U93631|GABAA receptor ligand

U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.

Product Name: U 93631|Cat No: DC9958|cas: 152273-12-6|Other Names: U-93631; U 93631

U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.In vitro: In the presence of U93631 at 5 UM, the peak amplitude decreased as a function of GABA concentration, with the half-maximal inhibitory concentration being approximately 100 nM, which is close to the Kd for the high affinity GABA site(85 nM). It appears that the drug interacts with GABA-bound receptors (at least monoliganded) and accelerates receptor desensitization,
rather than acting as an open channel blocker.

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

HMN-176|HMN176|mitosis inhibitor

HMN-176|HMN176|mitosis inhibitor

HMN-176 is a stilbene derivative which inhibits mitosis without significant effect on tubulin polymerization.

Product Name: HMN-176|Cat No: DC9957|cas: 173529-10-7|Other Names: HMN 176; HMN176

HMN-176 is a stilbene derivative which inhibits mitosis without significant effect on tubulin polymerization.In vitro: HMN-176 (2.5 μM) greatly increases the duration of mitosis in hTERT-RPE1 and CFPAC-1 Cell lines. The effect of HMN-176 on spindle morphology does not appear to be related to effects on microtubule polymerization. HMN-176 (2.5, 0.25, and 0.025 μM) inhibits aster formation in a concentration dependent manner[1]. HMN-176 (0.1, 1.0, or 10.0 μg/ml) demonstrates inhibitory effects in multiple tumors, with notable activity seen in breast, nonsmall-cell lung, and ovarian cancer specimens. HMN-176 demonstrates activity towards 63% of the breast (5/8), 67% of the non-small cell lung (4/6), and 57% of the ovarian (4/7) tumor specimens treated with 10.0 μg/ml[2]. HMN-176 shows potent cytotoxicity, with a mean IC50 value of 118 nM. HMN-176 displays similar cytotoxicity against tumors with various characteristics from different organs[3]. Treatment with 3 μM HMN-176 suppresses the expression of MDR1 mRNA by 56%. HMN-176 has no significant effect on the residual promoter activity.
In vivo: HMN-176 prevents spindle assembly and meiosis in Spisula oocytes by inhibiting centrosome-dependent MT nucleation, i.e., aster formation. Oocytes treated with 0.25 μM HMN-176 undergoes GVBD, but asters or spindles fails to form, even after prolonged periods. After p.o. of HMN-214 to male rats, the prodrug is not detected in the plasma, while plasma levels of HMN-176 peaks at 2 h and gradually decreases thereafter.

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

BFH772|BFH-772|VEGFR2 inhibitor

BFH772|BFH-772|VEGFR2 inhibitor

BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM.

Product Name: BFH772|Cat No: DC9956|cas: 890128-81-1|Other Names: BFH-772; BFH 772

BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM.InVitro: BFH772 is highly selective; apart from inhibiting VEGFR2 at 3 nM IC50, it also targets B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 is inactive (IC50>10 μM; >2 μM for cKIT) against all other tyrosine specific- and serine/threonine-specific protein kinases tested. BFH772  inhibits VEGFR2 with IC50 of 4.6±0.6 nM in CHO cells. BFH772  inhibits VEGFR2 with IC50 of 3 nM in HUVEC cells. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM. BFH772 is selective (IC50 values >0.5 μM) against the kinases of EGFR, ERBB2, INS-R, and IGF-1R and against the cytoplasmic BCR-ABL kinase. IC50 of BFH772 (<0.01 nM, n=2) demonstrates that they abrogated VEGF induced proliferation at remarkably low nM concentrations.
InVivo: BFH772 at 3 mg/kg orally dosed once per day potently inhibits melanoma growth (by 54-90% for primary tumor and 71-96% for metastasis growth) as depicted by treatment to control ratios. Dose–response curves of BFH772 at 0.3, 1, and 3 mg/kg demonstrate that even at the lowest concentrations, this naphthalene-1-carboxamide inhibits VEGF induced tissue weight and TIE-2 levels but only reaches statistical significance at 1 mg/kg and above.

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

BCL6 inhibitor(CID5721353)|CID-5721353

BCL6 inhibitor(CID5721353)|CID-5721353

CID5721353 is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor).

Product Name: BCL6 inhibitor(CID5721353)|Cat No: DC9955|cas: 301356-95-6|Other Names: CID 5721353,CID-5721353,CID 5721353

CID5721353 is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor).

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

A804598|A-804598|P2X7 receptor antagonist

A804598|A-804598|P2X7 receptor antagonist

A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.

Product Name: A 804598|Cat No: DC9954|cas: 1125758-85-1|Other Names: A 804598; A804598

A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.
In vitro: A-804598 potently blocked IL-1β release in the THP-1 cells (IC50 of 8.5 nM). A-804598 also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50 of 8.1 nM) with similar potency as in the calcium-influx assay.In vivo: Autoradiographic analysis of coronal rat brain sections revealed that there was specific binding of [3H]-A-804598 throughout the rat brain. High levels of [3H]-A-804598 specific binding were also found in the grey matter of the L4-L6 region of the rat spinal cord.

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

Leukadherin 1|Leukadherin1|agonist of CR3

Leukadherin 1|Leukadherin1|agonist of CR3

Leukadherin-1 is a specific agonist of CR3 and the leukocyte surface integrin CD11b/CD18.

Product Name: Leukadherin-1 |Cat No: DC9953|cas: 344897-95-6|Other Names: Leukadherin 1,Leukadherin1

Leukadherin-1 is a specific agonist of CR3 and the leukocyte surface integrin CD11b/CD18.In vitro: Leukadherin‐1 (LA1) modulates natural killer (NK) cell inflammatory cytokine secretion. The SLE-associated CD11b‐R77H variant does not influence NK cell response to Leukadherin-1. Leukadherin-1 does not modulate Syk activation in NK cells. Leukadherin-1 does not modulate Syk activation in NK cells. Leukadherin-1 (LA1) does not modulate signal transducer and activator of transcription (STAT)-4 phosphorylation. Leukadherin-1 modulates TLR-2 and TLR-7/8-induced monocyte cytokine secretion.
In vivo: Leukadherin-1 decreases macrophage infiltration in the lungs during hyperoxia. Furthermore, treatment with Leukadherin-1 improves alveolarization and angiogenesis and decreases pulmonary vascular remodeling and PH. Targeting leukocyte trafficking using Leukadherin-1, an integrin agonist, is beneficial in preventing lung inflammation and protecting alveolar and vascular structures during hyperoxia.

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

IQ-1 ,IQ1|cas 331001-62-8

IQ-1 ,IQ1|cas 331001-62-8

IQ-1 has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on.

Product Name: IQ-1 |Cat No: DC9952|cas: 331001-62-8|Other Names: IQ 1; IQ1

IQ-1 has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on.
1、IQ-1 maintains the pluripotency of murine ESCs in long-term culture in a Wnt-dependent manner.
2、IQ-1 decreased Wnt-stimulated phosphorylation of p300 at Ser-89.
3、 IQ-1 binds to serine/threonine phosphatase PP2A and prevents PP2A/Nkd interaction.
4、The binding of IQ-1 to PR72/130 leads to decreased phosphorylation of the coactivator protein p300 at Ser-89.
5、IQ-1 thereby diminishes the β-catenin/p300 interaction and prevents β-catenin coactivator switching from CBP to p300.

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

Wnt agonist 1(BML-284)|BML284|cas 853220-52-7

Wnt agonist 1(BML-284)|BML284|cas 853220-52-7

BML-284 is potent selective, and cell-permeable Wnt signaling activator.

Product Name: Wnt agonist 1(BML-284)|Cat No: DC9951|cas: 853220-52-7|Other Names: BML 284; BML284

BML-284 is potent selective, and cell-permeable Wnt signaling activator.in vitro: BML-284 induces the β-catenin/TCF-dependent reporter in a dose-dependent manner.
in vivio: BML-284 appears to mimic the effects of a Wnt ligand in a Xenopus model and may be a useful tool in the study of physiological processes that involve the Wnt pathway.

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

SU5614|SU-5614|FLT3 inhibitor

SU5614|SU-5614|FLT3 inhibitor

SU5614 is a potent and selective FLT3 inhibitor.

Product Name: SU5614|Cat No: DC9950|cas: 1055412-47-9|Other Names: SU 5614,SU-5614

SU5614 is a potent and selective FLT3 inhibitor. SU5614 reverts the antiapoptotic and pro-proliferative activity of FLT3 ligand (FL) in FL-dependent cells.

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

DprE1-IN-2|DprE1 inhibitor-2|cas 1615713-87-5

DprE1-IN-2|DprE1 inhibitor-2|cas 1615713-87-5

DprE1-IN-2 is a potent DprE1 inhibitor.

Product Name: DprE1-IN-2|Cat No: DC9949|cas: 1615713-87-5|Other Names: DprE1 inhibitor 2,DprE1 IN 2

DprE1-IN-2 is a potent DprE1 inhibitor. DprE1-IN-2 demonstrats efficacy in a rodent model of tuberculosis, making it promising for further development.

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

SNX-5422(PF04929113)| Hsp90/Her-2 degradation inhibitor

SNX-5422(PF04929113)| Hsp90/Her-2 degradation inhibitor

PF-04929113 (SNX-5422) is a potent and selective Hsp90 inhibitor (Kd of 41 nM). PF-04929113 also inhibits Her-2 degradation (IC50 of 37 nM).

Product Name: SNX-5422(PF04929113)|Cat No: DC9948|cas: 908115-27-5|Other Names: SNX5422,PF 04929113,SNX 5422,PF-04929113,

PF-04929113 (SNX-5422) is a potent and selective Hsp90 inhibitor (Kd of 41 nM). PF-04929113 also inhibits Her-2 degradation (IC50 of 37 nM). PF-04929113 is a small-molecule Hsp90 inhibitor based on the 6,7-dihydro-indazol-4-one scaffold. PF-04929113 exhibits potent effects on Her-2 stability and causes expected up-regulation of Hsp70. PF-04929113 shows potent antiproliferative activity against a broad range of cancer cell types, e.g. MCF-7 (IC50=16 nM), SW620 (IC50 of 19 nM), K562 (IC50 of 23 nM), SK-MEL-5 (IC50 of 25 nM), and A375 (IC50 of 51 nM).

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

RU43044,RU-43044|Glucocorticoid receptor antagonist

RU43044,RU-43044|Glucocorticoid receptor antagonist

The antiglucocorticoid RU43044 exerted significant agonist activity and activated MMTV-Luc transcription in osteosarcoma cells but not human breast cancer cells.

Product Name: RU43044|Cat No: DC9947|cas: 136959-96-1|Other Names: RU 43044,RU-43044

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

Lanabecestat|AZD3293|LY-3314814|BACE1 inhibitor

Lanabecestat|AZD3293|LY-3314814|BACE1 inhibitor

AZD3293 is a potent and selective orally active, brain-permeable BACE1 inhibitor,currently in development as a potential treatment for early Alzheimer’s disease.

Product Name: Lanabecestat(AZD3293,LY-3314814)|Cat No: DC9946|cas: 1383982-64-6|Other Names: AZD 3293,LY3314814,AZD-3293,LY 3314814

AZD3293 is an, orally administered, inhibitor of BACE1, the β-secretase sheddase that cleaves the APP protein to release APP's C99 fragment. This fragment then becomes a substrate for subsequent γ-secretase cleavage and Aβ peptide generation. The rationale is that inhibiting BACE1 will reduce amyloid-related toxicity in Alzheimer's disease. AZD3293 is one of several BACE1/2 inhibitors currently in development.

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

NSC-12|NSC12|small-molecule FGF trap

NSC-12|NSC12|small-molecule FGF trap

NSC12 is a PTX3-derived anti-FGF small molecule, inhibits FGF-dependent tumor growth, angiogenesis, and metastases,acts as a small-molecule FGF trap in cancer therapy.

Product Name: NSC-12|Cat No: DC9945|cas: 102586-30-1|Other Names: NSC-12,NSC 12,NSC12

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

GSK2292767|GSK-2292767|PI3Kδ inhibitor

GSK2292767|GSK-2292767|PI3Kδ inhibitor

GSK2292767 is a potent and selective PI3Kδ inhibitor.

Product Name: GSK2292767|Cat No: DC9944|cas: 1254036-66-2|Other Names: GSK 2292767,GSK-2292767

GSK2292767 is highly selective for PI3Kδ over the closely related isoforms and is active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation.

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

GSK2269557|GSK-2269557|PI3Kδ inhibitor

GSK2269557|GSK-2269557|PI3Kδ inhibitor

GSK-2269557 is a potent and selective PI3Kδ inhibitor over the closely related isoforms.

Product Name: GSK2269557|Cat No: DC9943|cas: 1254036-71-9|Other Names: GSK 2269557,GSK-2269557

GSK-2269557 is active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation. PI3Kδ is highly enriched in leukocytes, making it an attractive target for the treatment of inflammatory conditions, such as asthma,6 chronic obstructive pulmonary disease (COPD), and autoimmune diseases.

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

GDC-0853|RG7845|BTK inhibitor

GDC-0853|RG7845|BTK inhibitor

GDC-0853 is orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.

Product Name: GDC-0853(RG7845)|Cat No: DC9942|cas: 1434048-34-6 |Other Names: GDC-0853,RG7845,GDC0853,RG 7845,GDC 0853,RG-7845

GDC-0853 is orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, GDC-0853 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways, which leads to the inhibition of the growth of malignant B-cells that overexpress BTK. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B-lymphocyte development, activation, signaling, proliferation and survival.

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

XMD16-5|XMD16 5|TNK2 inhibitor

XMD16-5|XMD16 5|TNK2 inhibitor

XMD16-5 is a novel TNK2 inhibitor.

Product Name: XMD16-5|Cat No: DC9941|cas: N/A|Other Names: XMD 16-5,XMD-16-5,XMD 16 5

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

XMD8-87|XMD8 87|TNK2 inhibitor

XMD8-87|XMD8 87|TNK2 inhibitor

XMD8-87 is a novel TNK2 inhibitor.

Product Name: XMD8-87|Cat No: DC9940|cas: N/A|Other Names: XMD-8-87,XMD8 87,XMD 8 87

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

BAY 1082439|BAY1082439|PI3Kα/β inhibitor

BAY 1082439|BAY1082439|PI3Kα/β inhibitor

BAY 1082439 is a highly selective and balanced PI3Kα/β inhibitor demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN.

Product Name: BAY 1082439|Cat No: DC9939|cas: 1375469-38-7|Other Names: BAY10-82439; BAY 10-82439; BAY-10-82439; BAY1082439; BAY 1082439; BAY-1082439

BAY 1082439 has an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM), and >1000-fold selectivity against mTOR kinase. The balanced PI3Kα and PI3Kα activity of BAY 1082439 is also reflected in cellular mechanistic (p-AKT473) and proliferation assays in PI3Kα- (KPL4, BT474) vs. PI3Kα-driven (PC3, LNCaP) tumor cells. In vivo, BAY 1082439 showed clear advantages over the strong PI3Kα inhibitor BAY 80-6946 in PTEN/PI3Kα-driven tumor models (e.g., PC3 and HEC-1B), when the two compounds were compared at their MTDs. Furthermore, BAY 1082439 has unique pharmacokinetic (PK) properties with very high plasma free fractions across all species tested (33-50%), large Vss, high clearance and intermediate T1/2.

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

Lusutrombopag|S-888711|TPO receptor agonist

Lusutrombopag|S-888711|TPO receptor agonist

Lusutrombopag(S-888711) is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist being developed by Shionogi for chronic liver disease (CLD) patients with thrombocytopenia prior to elective invasive surgery.

Product Name: Lusutrombopag(S-888711)|Cat No: DC9938|cas: 1110766-97-6 |Other Names: S888711,S 888711

Lusutrombopag, also known as S-888711, is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist being developed by Shionogi for chronic liver disease (CLD) patients with thrombocytopenia prior to elective invasive surgery. Lusutrombopag acts selectively on the human TPO receptor and activates signal transduction pathways that promote the proliferation and differentiation of bone marrow cells into megakaryocytes, thereby increasing platelet levels. In September 2015, lusutrombopag received its first global approval in Japan for the improvement of CLD-associated thrombocytopenia in patients scheduled to undergo elective invasive procedures.

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

BMT145027,BMT-145027|mGluR5 PAM

BMT145027,BMT-145027|mGluR5 PAM

BMT-145027 is a potent mGluR5 PAM with no inherent mGluR5 agonist activity.

Product Name: BMT-145027|Cat No: DC9937|cas: N/A|Other Names: BMT145027,BMT 145027

BMT-145027 is a potent mGluR5 PAM with no inherent mGluR5 agonist activity. BMT-145027 is a non-MPEP site PAM to demonstrate in vivo efficacy. BMT-145027 has mGluR5 PAM EC50 = 47 nM, with fold shit = 3.5, and is effective in mouse NOR. The metabotropic glutamate receptor 5 (mGluR5) is an attractive target for the treatment of schizophrenia due to its role in regulating glutamatergic signaling in association with the N-methyl-D-aspartate receptor (NMDAR).

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

NMS-P118|PARP-1 inhibitor|CAS 1262417-51-5

NMS-P118|PARP-1 inhibitor|CAS 1262417-51-5

NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor with excellent ADME and pharmacokinetic profiles and high efficacy in vivo.

Product Name: NMS-P118|Cat No: DC9936|cas: 1262417-51-5|Other Names: NMS-P118; NMS-P 118; NMS P118

NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor with excellent ADME and pharmacokinetic profiles and high efficacy in vivo both as a single agent and in combination with Temozolomide in MDA-MB-436 and Capan-1 xenograft models, respectively. NMS-P118 was found to be less myelotoxic in vitro than olaparib (now marketed as Lynparza), a dual PARP-1/-2 inhibitor. NMS-P118 is the PARP-1 selective inhibitor with demonstrated anticancer activity as single agent, as well as in combination.

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

Basmisanil(RG1662,RG-1662)|cas 1159600-41-5

Basmisanil(RG1662,RG-1662)|cas 1159600-41-5

Basmisanil is a highly selective inverse agonist/negative allosteric modulator of α5 subunit-containing GABAA receptors which is under development by Roche for the treatment of cognitive impairment associated with Down syndrome.

Product Name: Basmisanil(RG1662)|Cat No: DC9935|cas: 1159600-41-5 |Other Names: RG 1662; RG-1662; RG1662; RO5186582; RO-5186582; RO 5186582; Basmisanil

Basmisanil, also known as RG1662, RO5186582, is a highly selective inverse agonist/negative allosteric modulator of α5 subunit-containing GABAA receptors which is under development by Roche for the treatment of cognitive impairment associated with Down syndrome. As of August 2015, it is in phase II clinical trials for this indication. Down syndrome (DS) is the most commonly identifiable genetic form of intellectual disability. Individuals with DS have considerable deficits in intellectual functioning (i.e., low intellectual quotient, delayed learning and/or impaired language development) and adaptive behavior.

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

FGFR4-IN-1|cas 1708971-72-5

FGFR4-IN-1|cas 1708971-72-5

FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.

Product Name: FGFR4-IN-1 |Cat No: DC9933|cas: 1708971-72-5|Other Names:

FGFR4-IN-1 significantly inhibits the proliferation of HuH-7 hepatocellular carcinoma cells with IC50 of 7.8 nM.

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

YL-0919|YL0919|5-HT1A Receptor Agonist

YL-0919|YL0919|5-HT1A Receptor Agonist

YL-0919 is a novel synthetic compound with combined high affinity and selectivity for serotonin transporter and 5-HT1A receptors.

Product Name: YL-0919 |Cat No: DC9932|cas: 1339058-04-6 |Other Names: YL0919 ,YL 0919

YL-0919 is a novel synthetic compound with combined high affinity and selectivity for serotonin transporter and 5-HT1A receptors.

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

2016年12月28日星期三

Compound 4| cas 132819-92-2

Compound 4| cas 132819-92-2

Product Name: Compound 4|Cat No: DC9930|cas: 132819-92-2|Other Names: Compound 4

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

JK184,JK-184||Hh signaling inhibitor

JK184,JK-184||Hh signaling inhibitor

JK-184  is a potent downstream hedgehog (Hh) signaling inhibitor that prevents Gli-dependent transcriptional activity (IC50 = 30 nM).

Product Name: JK-184|Cat No: DC9929|cas: 315703-52-7|Other Names: JK184, JK-184

Potent downstream hedgehog (Hh) signaling inhibitor that prevents Gli-dependent transcriptional activity (IC50 = 30 nM). Exhibits antiproliferative activity in a range of cancer cell lines (GI50 = 3 - 21 nM) and in human xenografts in vivo. Inhibits alcohol dehydrogenase 7 (Adh7) (IC50 = 210 nM) and acts as a microtubule depolymerizing agent in vitro.

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

VU 0364770|mGlu4 positive allosteric modulator

VU 0364770|mGlu4 positive allosteric modulator

VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.

Product Name: VU 0364770|Cat No: DC9928|cas: 61350-00-3|Other Names: VU0364770,VU-0364770

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

ON1231320|ON-1231320|PLK2 inhibitor|131247-39-8

ON1231320|ON-1231320|PLK2 inhibitor|131247-39-8

ON1231320 is a potent selective inhibitor of Polo like kinase 2 (PLK2).

Product Name: ON1231320|Cat No: DC9927|cas: 131247-39-8|Other Names: ON 1231320,ON-1231320

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

XMU-MP-1|MST1/2 inhibitor

XMU-MP-1|MST1/2 inhibitor

XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50 values of 71.1 ± 12.9 nM and 38.1 ± 6.9 nM against MST1 and MST2, respectively.

Product Name: XMU-MP-1|Cat No: DC9926|cas: N/A|Other Names:

XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50 values of 71.1 ± 12.9 nM and 38.1 ± 6.9 nM against MST1 and MST2, respectively. XMU-MP-1 also reduces the phosphorylation of LATS1/2, and YAP by inhibiting MST1/2 kinase activities.
In vitro: XMU-MP-1 is on-target to MST1/2. XMU-MP-1 block MST1/2 kinase activities, thereby activating the downstream effector Yes-associated protein and promoting cell growth. XMU-MP-1 is dissolved in DMSO (stock concentration, 10 mM).
In vivo: XMU-MP-1 displayed excellent in vivo pharmacokinetics and is able to augment mouse intestinal repair, as well as liver repair and regeneration, in both acute and chronic liver injury mouse models at a dose of 1 to 3 mg/kg via intraperitoneal injection. XMUMP-1 treatment exhibit substantially greater repopulation rate of human hepatocytes in the Fah-deficient mouse model than in the vehicle-treated control, indicating that XMU-MP-1 treatment might facilitate human liver regeneration.
XMUMP-1 is dissolved in 0.1% citric acid aqueous solution containing 20% Kolliphor HS 15.

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

PP2 analog|Src kinase inhibitor|309739-67-1

PP2 analog|Src kinase inhibitor|309739-67-1

PP2 analog is the analog of PP2,a Src family kinase inhibitor.

Product Name: PP2 analog|Cat No: DC9931|cas: 309739-67-1|Other Names: PP 2 analog,PP-2 analog

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


CXD101(AZD-9468)|HDAC inhibitor

CXD101(AZD-9468)|HDAC inhibitor

CXD101(AZD-9468) is a novel histone deacetylase (HDAC) inhibitor with potential antineoplastic activity.

Product Name: CXD101(AZD-9468)|Cat No: DC9925|cas: N/A|Other Names: CXD 101,AZD9468,CXD-101,AZD 9468

CXD101 is a novel histone deacetylase (HDAC) inhibitor with potential antineoplastic activity. Although the exact therapeutic mechanism of action for CXD101 is not known, oral administration of this agent should inhibit the catalytic activity of HDAC, which results in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling and an altered pattern of gene expression.

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

SB 218078|SB218078|Chk1 inhibitor

SB 218078|SB218078|Chk1 inhibitor

SB218078 is an inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively).

Product Name: SB218078|Cat No: DC9924|cas: 135897-06-2|Other Names: SB 218078,SB-218078

SB218078 is an inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively). Abrogates G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition. Potentiates cytotoxicity of DNA-damaging drugs, enhancing the efficacy of some chemotherapeutics.

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

CeMMEC1|TAF1 bromodomain inhibitor|440662-09-9

CeMMEC1|TAF1 bromodomain inhibitor|440662-09-9

CeMMEC1 is a novel potent inhibitor of the second bromodomain of TAF1, binding neither the first nor the second bromodomain of BRD4.

Product Name: CeMMEC1|Cat No: DC9923|cas: 440662-09-9|Other Names:

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

Macranthoidin B|cas 136849-88-2|Supplied by DC Chem

Macranthoidin B|cas 136849-88-2|Supplied by DC Chem

Macranthoidin B is a major bioactive saponin in rat plasma after oral administration of extraction of saponins from Flos Lonicerae.

Product Name: Macranthoidin B|Cat No: DC9922|cas: 136849-88-2|Other Names:

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

Hederacoside C|cas 14216-03-6|Supplied by DC Chem

Hederacoside C|cas 14216-03-6|Supplied by DC Chem

Hederacoside C is a principal bioactive pharmaceutical ingredient of Hedera helix leaf that can treat respiratory disorders, because of its expectorant, bronchodilator, antibacterial, and bronchospasmolytic effects.

Product Name: Hederacoside C|Cat No: DC9921|cas: 14216-03-6|Other Names:

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

alpha-Hederin|cas 27013-91-8|Supplied by DC Chem

alpha-Hederin|cas 27013-91-8|Supplied by DC Chem

alpha-hederin is a water-soluble pentacyclic triterpenoid saponin, possessing several biological properties such as antispasmodic, moliscicidic, anthelmithic and inhibiting cell proliferation.

Product Name: alpha-Hederin|Cat No: DC9920|cas: 27013-91-8|Other Names:

alpha-hederin is a water-soluble pentacyclic triterpenoid saponin, possessing several biological properties such as antispasmodic, moliscicidic, anthelmithic and inhibiting cell proliferation.
In vitro: a-hederin is cytotoxic and inhibits proliferation in both
cel lines at rather low concentrations. , a-hederin reduces the
mitotic activity in treated cels.
In vivo: alpha-hederin had preventive effect on sensitized rats like thymoquinone. It may intervene in miRNA-126 expression, which consequently could interfere with IL-13 secretion pathway leading to a reduction in inflammatory responses.

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


Pulchinenoside A|cas 129724-84-1|Supplied by DC Chem

Pulchinenoside A|cas 129724-84-1|Supplied by DC Chem

Pulchinenoside A|cas 129724-84-1|Supplied by DC Chem

Pulchinenoside A is a natural triterpenoid saponin that enhances synaptic plasticity in the adult mouse hippocampus and facilitates spatial memory in adult mice.

Product Name: Pulchinenoside A|Cat No: DC9919|cas: 129724-84-1|Other Names:

Pulchinenoside A is a natural triterpenoid saponin that enhances synaptic plasticity in the adult mouse hippocampus and facilitates spatial memory in adult mice.
In vitro: Additions of pulsatilloside A and anemoside A3, at dosages ranging from 0.1, 1 and 10 μg/ml, protected PC12 cells from apoptosis.
In vivo:AA3 also acts as a non-competitive NMDA receptor (NMDAR) modulator with a neuroprotective capacity against ischemic brain injury and overexcitation in rats. Anemoside A3 produces relaxation in rat renal arteries through multiple mechanisms.

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

Gracillin|cas 19083-00-2|Supplied by DC Chem

Gracillin|cas 19083-00-2|Supplied by DC Chem

Gracillin is a kind of steroidal saponin isolated from the root bark of wild yam Dioscorea nipponica with antitumor agent.

Product Name: Gracillin|Cat No: DC9918|cas: 19083-00-2|Other Names:

Gracillin is a kind of steroidal saponin isolated from the root bark of wild yam Dioscorea nipponica with antitumor agent.
Gracillin could induce cell cycle arrest, oxidative stress, and apoptosis in HL60 cells.

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

Acacetin|cas 480-44-4|Supplied by DC Chem

Acacetin|cas 480-44-4|Supplied by DC Chem

Acacetin is an O-methylated flavone found in Robinia pseudoacacia (black locust), Turnera diffusa (damiana),Betula pendula (silver birch),and in the fern Asplenium normale.

Product Name: Acacetin|Cat No: DC9917|cas: 480-44-4|Other Names:

Natural acacetin was a 4.0-fold and 5.5-fold more potent inhibitor of BACE-1 than oleanolic acid and maslinic acid, respectively.
Acacetin significantly suppressed the photoreceptor collapse.
Acacetin significantly reduces the Aβ levels by interfering with human APP proteolytic processing and BACE-1 expression.
Acacetin inhibited the generation of the APP-CTF by affecting APP cleavage.
Acacetin prolongs lifespan of significantly in the dose dependent manner. Acacetin
(25 uM) had the greatest effect on longevity, extending mean lifespan significantly by 27.31% at 25 uM concentration

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

Quillaic acid(Quillaja sapogenin)|cas 631-01-6

Quillaic acid(Quillaja sapogenin)|cas 631-01-6

Quillaic acid(Quillaja sapogenin) is the major aglycone of the widely studied saponins of the Chilean indigenous tree Quillaja saponaria Mol; can elicit dose-dependent antinociceptive effects in two murine thermal models.

Product Name: Quillaic acid(Quillaja sapogenin)|Cat No: DC9916|cas: 631-01-6|Other Names:

Quillaic acid(Quillaja sapogenin) is the major aglycone of the widely studied saponins of the Chilean indigenous tree Quillaja saponaria Mol; can elicit dose-dependent antinociceptive effects in two murine thermal models.

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

PF-04995274|PF04995274|5-HT4 receptor agonist

PF-04995274|PF04995274|5-HT4 receptor agonist

PF-04995274 is a 5-HT4 receptor partial agonist. It thought to act centrally as a pro-cognitive agent that being developed for the treatment of Alzheimer's disease (AD).

Product Name: PF-04995274|Cat No: DC9915|cas: 1331782-27-4|Other Names: PF04995274,PF 04995274

PF-04995274 is a 5-HT4 receptor partial agonist. It thought to act centrally as a pro-cognitive agent that being developed for the treatment of Alzheimer's disease (AD).

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

Bruceantin(NSC165563) |cas 41451-75-6

Bruceantin(NSC165563) |cas 41451-75-6

Bruceantin(NSC165563) is first isolated from Brucea antidysenterica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.

Product Name: Bruceantin(NSC165563) |Cat No: DC9914|cas: 41451-75-6|Other Names:

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

Hypericin|548-04-9|anticancer/antidepressant agent

Hypericin|548-04-9|anticancer/antidepressant agent

Hypericin is a photosensitive antiviral with anticancer and antidepressant agent derived from Hypericum perforatum. It can inhibit tyrosine kinases with IC50 of 7.5 μM.

Product Name: Hypericin|Cat No: DC9913|cas: 548-04-9|Other Names:

Hypericin is a photosensitive antiviral with anticancer and antidepressant agent derived from Hypericum perforatum. It can inhibit tyrosine kinases with IC50 of 7.5 μM.
In vitro:The photosensitive of hypericin can induce both apoptosis and necrosis in a concentration and light dose-dependent fashion. PDT with hypericin results in the activation of multiple pathways that can either promote or counteract the cell death program. It can effect cytotoxic to tumor cells by visible light.

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

Echinocystic acid|cas 510-30-5|Supplied by DC Chem

Echinocystic acid|cas 510-30-5|Supplied by DC Chem

Echinocystic acid  a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory and anti-tumor properties.

Product Name: Echinocystic acid|Cat No: DC9912|cas: 510-30-5|Other Names:

Echinocystic acid  a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory and anti-tumor properties.
In vitro: Echinocystic acid (EA) inhibit the formation of osteoclast. EA inhibit RANKL-induced NF-κB activation and ERK phosphorylation in BMMs. [EA inhibit IL-1β-induced inflammation in chondrocytes.
In vivo: Echinocystic acid reduces reserpine-induced pain/depression dyad in mice.


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

Pulsatilla saponin D(SB365)|chemopreventive agent

Pulsatilla saponin D(SB365)|chemopreventive agent

Pulsatilla saponin D(SB365) isolated from the root of Pulsatilla koreana, has exhibited potential beneficial effects as a chemopreventive agent for critical health conditions including cancer.

Product Name: Pulsatilla saponin D(SB365)|Cat No: DC9911|cas: 68027-15-6 (848784-85-0)|Other Names: SB365; SB 365; SB-365; Hederacolchiside A

SB365 effectively inhibited the growth of gastric cancer cells. Its apoptotic effect was accompanied by increased evidence of cleaved caspase-3 and poly(ADP ribose) polymerase. To elucidate the anticancer mechanism of SB365, we used an array of 42 different receptor tyrosine kinases (RTKs). Of the 42 different phospho-RTKs, SB365 strongly inhibited expression of activated c-mesenchymal-epithelial transition factor (c-Met) in gastric cancer cells. SB365 strongly suppressed the growth and proliferation of 5 human pancreatic cancer cell lines (MIAPaCa-2, BXPC-3, PANC-1, AsPC-1 and HPAC). The apoptotic effect of SB365 was demonstrated by increased levels of cleaved caspase-3 and decreased Bcl-2 expression via mitochondrial membrane potential, as well as elevated numbers of terminal deoxynucleotidyl-transferase-mediated dUTP nick end labeling (TUNEL)-positive apoptotic cells [2]. SB365 strongly suppressed the growth and proliferation of colon cancer cells and induced their apoptosis. Also, SB365 showed anti-angiogenic activity by decreasing the expression of HIF-1α and VEGF. These results were confirmed by an in vivo study showing that SB365 significantly inhibited tumor growth by the induction of apoptosis and inhibition of angiogenesis with stronger anticancer activity than 5-FU.

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

CYCLOPAMINE|cas 4449-51-8|supplier DC Chemicals

CYCLOPAMINE|cas 4449-51-8|supplier DC Chemicals

Cyclopamine(11-Deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM.

Product Name: CYCLOPAMINE|Cat No: DC9910|cas: 4449-51-8|Other Names: N/A

Cyclopamine(11-Deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM.
in vitro: Cyclopamine inhibits the Hedgehog signaling pathway with an IC50 of 46 nM, and blocks the activity of human Smo receptor expressed in CHO-K1 cells in [3H]Hh-Ag binding assay with an IC50 of 280 nM. Cyclopamine significantly inhibits Hedgehog pathway activity in a dose-dependent manner in gut-derived tumor cell lines expressing Patched (PTCH) mRNA, and induces growth inhibition of those tumor cell lines by 75-95% at the concentration of 3 μM, but ineffective towards the colon tumor cells without PTCH mRNA expression, suggesting the effects of Cyclopamine treatment are Hedgehog pathway related rather than generally cytotoxic. By blocking Hedgehog signaling through direct interaction with Smo, Cyclopamine (10 μM) inhibits the proliferation of SMOhigh Cyclopamine-responsive cell lines L3.6sl and Panc 05.04 by 75-80%, and increases the apoptosis by 2.5- to 3.5-fold, without affecting the BxPC3-SMOlow cell line .Cyclopamine treatment significantly decreases of Snail mRNA and increasea E-cadherin transcripts in the E3LZ10.7 cell line. Independent of inhibition of cell growth, Cyclopamine treatment significantly inhibits the invasive phenotype of Hedgehog-dependent L3.6pl cells, causing a >500-fold reduction in the number of transmigrating cells, but not that of the Hedgehog-independent cell line Panc-1.
in vivo: Administration of Cyclopamine at dose of 50 mg/kg/day for 22 days eradicates the HUCCT1 xenografts in mice with no obvious adverse effects. Cyclopamine treatment at dose of 1.2 mg for 7 days induces significant apoptosis of tumor cells and decreases the tumor mass by 50-60% in Panc 05.04- and L3.6sl-derived tumors, respectively, but not in the BxPC3-SMOlow tumors. Administration of Cyclopamine alone profoundly inhibits tumor metastases in xenografts of E3LZ10.7 and L3.6pl, and completely abrogates metastases when in combination of gemcitabine.

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


AM-2099|AM2099|NaV1.7 Inhibitor

AM-2099|AM2099|NaV1.7 Inhibitor

AM-2099 is a potent and selective NaV1.7 Inhibitor.

Product Name: AM2099|Cat No: DC9909|cas: 1443373-17-8 |Other Names: AM 2099,AM-2099

AM-2099 is a potent and selective NaV1.7 Inhibitor (hNav1.7 IC50 = 0.16 uM; hNav1.5 IC50 > 30 uM; Papp = 31 x 10 (-6)cm/s; Rat IV CL (b/h/kg) \= 0.54; cLogD = 2.1). AM-2099 demonstrated a favorable pharmacokinetic profile in rat and dog and demonstrated dose-dependent reduction of histamine-induced scratching bouts in a mouse behavioral model following oral dosing.

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

GNE-272|GNE272|Bromodomains CBP/EP300 probe

GNE-272|GNE272|Bromodomains CBP/EP300 probe

GNE-272 is a in Vivo Probe for the Bromodomains of CBP/EP300.

Product Name: GNE-272|Cat No: DC9934|cas: 1936428-93-1|Other Names: GNE272,GNE 272

GNE-272 is a potent and selective in Vivo Probe for the Bromodomains of CBP/EP300 (CBP IC50 = 0.02 μM, EP300 IC50 = 0.03 μM, BRET IC50 = 0.41 μM, BRD4(1) C50 = 13 μM).GNE-272 showed a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. CBP has also been implicated in neurological disorders where a CBP bromodomain inhibitor has been shown to reduce expression of a regulator of G-protein signaling (RGS4).

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

CPI-1205|CPI1205|EZH2 inhibitor

CPI-1205|CPI1205|EZH2 inhibitor

CPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2.

Product Name: CPI-1205|Cat No: DC9908|cas: 1621862-70-1 |Other Names: CPI 1205,CPI1205

CPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2. Upon oral administration, CPI-1205 selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 on lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells.

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

GSK9311|GSK-9311|BRPF bromodomain inhibitor

GSK9311|GSK-9311|BRPF bromodomain inhibitor

GSK9311 is a potent and highly selective inhibitor of the BRPF bromodomain (BRPDF1 pIC50 = 6.0; BRPDF2 pIC50 = 4.3).

Product Name: GSK9311|Cat No: DC9907|cas: 1923851-49-3|Other Names: GSK 9311,GSK-9311

GSK9311 is a potent and highly selective inhibitor of the BRPF bromodomain (BRPDF1 pIC50 = 6.0; BRPDF2 pIC50 = 4.3). The BRPF (Bromodomain and PHD Fingercontaining) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. BRPF1 (bromodomain and PHD finger containing protein 1) is involved in the epigenetic regulation of gene expression and have been implicated in human cancer.

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

K-Ras-IN-1|KRAS inhibitor|cas 84783-01-7

K-Ras-IN-1|KRAS inhibitor|cas 84783-01-7

K-Ras-IN-1 is a K-Ras inhibitor, by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.

Product Name: K-Ras-IN-1|Cat No: DC9906|cas: 84783-01-7|Other Names:

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

Wogonin|anti-inflammatory/COX-2 inhibitor

Wogonin|anti-inflammatory/COX-2 inhibitor

Wogonin is a cell-permeable and orally available flavonoid that displays anti-inflammatory and anticancer properties.

Product Name: Wogonin|Cat No: DC9905|cas: 632-85-9|Other Names:

Wogonin is an anti-inflammatory agent and COX-2 inhibitor, which inhibits the induction of both iNOS and COX-2. Wogonin inhibits COX-2 (IC50 = 46 uM) without affecting COX-1. Wogonin enhances antitumor activity of tumor necrosis factor-related apoptosis-inducing ligand in vivo through ROS-mediated downregulation of cFLIPL and IAP proteins.

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


GW0742|GW-0742|PPARδ agonistDC Chemicals

GW0742|GW-0742|PPARδ agonistDC Chemicals

GW-0742 is a potent and highly selective PPARδ agonist.

Product Name: GW0742|Cat No: DC9904|cas: 317318-84-6|Other Names: GW 0742,GW-0742

GW-0742 is a potent and highly selective PPARδ agonist. EC50 values are 0.001, 1.1 and 2 μM for transactivation of human PPARδ, -α, and -γ receptors respectively. Neuroprotective in rat cerebellar granule neuronal cultures after brief (12-hour) exposure but exhibits inherent toxicity after prolonged (48-hour) incubation. Increases rate of fatty acid oxidation and protects against ischemia/reperfusion injury in neonatal and adult cardiomyocytes.

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

Saccharin 1-methylimidazole (SMI)|cas 482333-74-4|DC Chemicals

Saccharin 1-methylimidazole (SMI)|cas 482333-74-4|DC Chemicals

SMI is considered a general-purpose activator for DNA and RNA synthesis.

Product Name: Saccharin 1-methylimidazole (SMI)|Cat No: DC9903|cas: 482333-74-4|Other Names:

SMI is considered a general-purpose activator for DNA and RNA synthesis.

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

PRIMA-1|cas 5608-24-2|DC Chemicals

PRIMA-1|cas 5608-24-2|DC Chemicals

PRIMA-1 is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.

Product Name: PRIMA-1|Cat No: DC9902|cas: 5608-24-2|Other Names:

PRIMA-1 is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.

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

Verubecestat (MK-8931)|1286770-55-5|BACE1 inhibitor

Verubecestat (MK-8931)|1286770-55-5|BACE1 inhibitor

MK-8931 is a BACE1 inhibitor. MK-8931  binds significantly to β-secretase.

Product Name: Verubecestat (MK-8931)|Cat No: DC9901|cas: 1286770-55-5|Other Names: MK8931,MK 8931,MK-8931

MK-8931 is a BACE1 inhibitor. MK-8931  binds significantly to β-secretase.

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

Acetaminophen|cas 103-90-2|DC Chemicals

Acetaminophen|cas 103-90-2|DC Chemicals

Acetaminophen is a COX inhibitor for COX-1 and COX-2 with IC50 of 113.7 μM and 25.8 μM, respectively.

Product Name: Acetaminophen|Cat No: DC9900|cas: 103-90-2|Other Names:

Acetaminophen is a COX inhibitor for COX-1 and COX-2 with IC50 of 113.7 μM and 25.8 μM, respectively.

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

VO-Ohpic|cas 476310-60-8|DC Chemicals

VO-Ohpic|cas 476310-60-8|DC Chemicals

VO-Ohpic is a potent inhibitor of PTEN (phosphatase and tensin homolog) with IC50 of 35 nM.

Product Name: VO-Ohpic|Cat No: DC9899|cas: 476310-60-8|Other Names:

VO-Ohpic is a potent inhibitor of PTEN (phosphatase and tensin homolog) with IC50 of 35 nM.

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

SIS3|cas 521984-48-5|DC Chemicals

SIS3|cas 521984-48-5|DC Chemicals

SIS3 is a potent and selective inhibitor of Smad3. a potent regulator of the human Nox4 promoter.

Product Name: SIS3|Cat No: DC9898|cas: 521984-48-5|Other Names:

SIS3 is a potent and selective inhibitor of Smad3. a potent regulator of the human Nox4 promoter.

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

Palmitoylethanolamide|cas 544-31-0|DC Chemicals

Palmitoylethanolamide|cas 544-31-0|DC Chemicals

Palmitoylethanolamide(PEA) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM.

Product Name: Palmitoylethanolamide|Cat No: DC9897|cas: 544-31-0|Other Names:

Palmitoylethanolamide(PEA) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM.

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


Cinnarizine|cas 298-57-7|DC Chemicals

Cinnarizine|cas 298-57-7|DC Chemicals

Cinnarizine is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker.

Product Name: Cinnarizine|Cat No: DC9896|cas: 298-57-7|Other Names:

Cinnarizine is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker.

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

L-Glutamic acid monosodium salt|cas 142-47-2|DC Chemicals

L-Glutamic acid monosodium salt|cas 142-47-2|DC Chemicals

L-Glutamic acid monosodium salt is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods.

Product Name: L-Glutamic acid monosodium salt|Cat No: DC9895|cas: 142-47-2|Other Names:

L-Glutamic acid monosodium salt is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods.

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

Acetylcholine iodide|cas 2260-50-6|DC Chemicals

Acetylcholine iodide|cas 2260-50-6|DC Chemicals

Acetylcholine iodide is a neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.

Product Name: Acetylcholine iodide|Cat No: DC9894|cas: 2260-50-6|Other Names:

Acetylcholine iodide is a neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.

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

Evans Blue|cas 314-13-6|DC Chemicals

Evans Blue|cas 314-13-6|DC Chemicals

Evans Blue is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist

Product Name: Evans Blue|Cat No: DC9893|cas: 314-13-6|Other Names:

Evans Blue is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist

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

3,3'-Diindolylmethane|cas 1968-05-4|DC Chemicals

3,3'-Diindolylmethane|cas 1968-05-4|DC Chemicals

3,3'-Diindolylmethane(DIM) is a major digestive product of indole-3-carbinol, a potential anticancer component of cruciferous vegetables.

Product Name: 3,3'-Diindolylmethane|Cat No: DC9892|cas: 1968-05-4|Other Names:

3,3'-Diindolylmethane(DIM) is a major digestive product of indole-3-carbinol, a potential anticancer component of cruciferous vegetables.

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

Isatin|cas 91-56-5|DC Chemicals

Isatin|cas 91-56-5|DC Chemicals

Isatin is an endogenous MAO inhibitor.

Product Name: Isatin|Cat No: DC9891|cas: 91-56-5|Other Names:

Isatin is an endogenous MAO inhibitor.

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


Diethyl maleate|cas 141-05-9|DC Chemicals

Diethyl maleate|cas 141-05-9|DC Chemicals

Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NFkB.

Product Name: Diethyl maleate|Cat No: DC9890|cas: 141-05-9|Other Names:

Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NFkB.

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

Kynurenic acid|cas 492-27-3|DC Chemicals

Kynurenic acid|cas 492-27-3|DC Chemicals

Kynurenic acid, a natural metabolite of tryptophan via the kynurenine pathway, is a broad-spectrum excitatory amino acid antagonist.

Product Name: Kynurenic acid|Cat No: DC9889|cas: 492-27-3|Other Names:

Kynurenic acid, a natural metabolite of tryptophan via the kynurenine pathway, is a broad-spectrum excitatory amino acid antagonist.

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

BI-9564|BI9564|BRD9/7 inhibitor

BI-9564|BI9564|BRD9/7 inhibitor

BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.

Product Name: BI-9564|Cat No: DC9888|cas: 1883429-22-8|Other Names: BI9564,BI 9564

BI-9564 (MW 353.4) is a BRD9 / 7 specific inhibitor that has been developed in collaboration with Boehringer Ingelheim. This probe was discovered through fragment-based screening and optimized by structure guided design. BI-9564 binds to BRD9 with a higher affinity (Kd=14 nM, ITC) than to BRD7 (Kd=239nM, ITC), is completely negative on BET family members (>100 µM by AlphaScreen) and demonstrates cellular activity by FRAP on BRD9 and BRD7 at 0.1 µM and 1 µM, respectively. BI-9564 shows off-target selectivity to CECR2 in vitro (258 nM, ITC), but not in cells (at 1 µM, FRAP).

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

FRAX1036|cas 1432908-05-8|DC Chemicals

FRAX1036|cas 1432908-05-8|DC Chemicals

FRAX1036 is a novel ATP-competitive small molecule inhibitor of group I p21-activated Kinases (PAKs).

Product Name: FRAX1036|Cat No: DC9887|cas: 1432908-05-8|Other Names:

FRAX1036 is a novel ATP-competitive small molecule inhibitor of group I p21-activated Kinases (PAKs).

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

D-(+)-Cellobiose|cas 528-50-7|DC Chemicals

D-(+)-Cellobiose|cas 528-50-7|DC Chemicals

D-(+)-Cellobiose is a substrate of β-glucosidase.

Product Name: D-(+)-Cellobiose|Cat No: DC9886|cas: 528-50-7|Other Names:

D-(+)-Cellobiose is a substrate of β-glucosidase.

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

Benzenesulfonamide|cas 98-10-2|DC Chemicals

Benzenesulfonamide|cas 98-10-2|DC Chemicals

Benzenesulfonamide ia an inhibitor of carbonic anhydrases

Product Name: Benzenesulfonamide|Cat No: DC9885|cas: 98-10-2|Other Names:

Benzenesulfonamide ia an inhibitor of carbonic anhydrases

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

Etretinate|cas 54350-48-0|DC Chemicals

Etretinate|cas 54350-48-0|DC Chemicals

Etretinate is an oral aromatic retinoid acid which is effective in psoriasis and other dermatological syndromes.

Product Name: Etretinate|Cat No: DC9884|cas: 54350-48-0|Other Names:

Etretinate is an oral aromatic retinoid acid which is effective in psoriasis and other dermatological syndromes. It activates retinoid receptors, causing an induction of cell differentiation, inhibition of cell proliferation, and inhibition of tissue infiltration by inflammatory cells.

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

WNK463|WNK-463|pan-WNK-kinase inhibitor

WNK463|WNK-463|pan-WNK-kinase inhibitor

WNK463 is a pan-WNK-kinase inhibitor. It potently inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4).

Product Name: WNK463|Cat No: DC9883|cas: 2012607-27-9|Other Names: WNK 463,WNK-463

WNK463 is a pan-WNK-kinase inhibitor. It potently inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4).

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

CeMMEC13|cas 1790895-25-8|DC Chemicals

CeMMEC13|cas 1790895-25-8|DC Chemicals

CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 µM).

Product Name: CeMMEC13|Cat No: DC9882|cas: 1790895-25-8|Other Names:

CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 µM).

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

RHPS4|cas 390362-78-4|DC Chemicals

RHPS4|cas 390362-78-4|DC Chemicals

RHPS4 is a potent inhibitor of Telomerase at submicromolar.

Product Name: RHPS4|Cat No: DC9881|cas: 390362-78-4|Other Names:

RHPS4 is a potent inhibitor of Telomerase at submicromolar.

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

KYA1797K|cas 1956356-56-1|DC Chemicals

KYA1797K|cas 1956356-56-1|DC Chemicals

KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).

Product Name: KYA1797K|Cat No: DC9880|cas: 1956356-56-1|Other Names:

KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).

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