NVP-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NVP-2 是一种有效的、选择性的、ATP 竞争性 CDK9 抑制剂，IC50 为 <0.514 nM (CDK9/CyclinT)。

NVP-2 is a?potent, selective, ATP-competitive CDK9 inhibitor with IC50 of <0.514 nM (CDK9/CyclinT); displays excellent kinome selectivity against a panel of 468 kinases, including CDK7 (IC50>10 uM) and CDK13; inhibits proliferation of MOLT4 cells with IC50 of 9 nM, inhibits phosphorylation of RNA Pol II CTD residues serine 2, 5 and 7, induces significant reductions in the mRNA levels of MYB and RUNX1 in MOLT4 cells.

NVP-2 has an anti-proliferation of leukemia cells, inhibits KOPT-K1, Jurkat, P12-ICHIKAWA, DU.528, MOLT 16, HSB-2, PF-382, SKW-3, SUP-T11, DND-41 and HPB-ALL cells with IC50 values of 0.1688 μM, 0.1233? μM,0.5736? μM,0.1575 μM, 0.1620 μM,0.1585 μM, 0.1808 μM, 0.2589 μM, 0.0918 μM and 0.3023 μM, respectively.NVP-2 (250 nM-1 μM; 6 hours) engages CDK9 in wildtype and CRBN/MOLT4 cells at all concentrations, while CDK2 and CDK7 are unaffected.NVP-2 (0-10 nM; 72 hours) exhibits CRBN-dependent anti-proliferative and pro-apoptotic effects in MOLT4 cells, displays an IC50 value of 9 nM.NVP-2 (250 nM; 24 hours) induces cell apoptosis in MOLT4 cells, upregulates caspase-3 and γH2A.X expression. However, while the compound washout significantly reduces the degree of apoptosis induced by NVP-2.Cell Viability Assay Cell Line:Leukemia cell lines Concentration:0.1233 μM-0.5736 μM Incubation Time:72 hours Result:Inhibited Leukemia cell lines viabity.Western Blot Analysis Cell Line:Wildtype and?CRBN?/??MOLT4 cells Concentration:1 μM; 500 nM; 250 nM Incubation Time:6 hoursResult:Degrade CDK9 ?sub-stoichiometrically at all concentrations. Apoptosis Analysis Cell Line:Wildtype and?CRBN?/??MOLT4 cells Concentration:250 nMIncubation Time:24 hoursResult:Induced cell apoptosis in cells and wash outed the compound relieved NVP-2-induced cell apoptosis.Cell Proliferation Assay Cell Line:MOLT4 cells Concentration:0-10 nM Incubation Time:72 hours Result:Exhibited anti-proliferative effects inMOLT4 cells.

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NVP2 | NVP 2 | CDK9 inhibitor

Angiogenesis

CDK

CDK

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1263373-43-8

513.083

C27H37ClN6O2

>98% (HPLC)

DMSO : ≥ 100 mg/mL 194.91 mM

N#CC1(CNC2=NC(C3=CC(N[C@H]4CC[C@H](N[C@H](C)COC)CC4)=NC=C3Cl)=CC=C2)CCOCC1

4-(((2'-chloro-5'-(((1R,4r)-4-(((R)-1-methoxypropan-2-yl)amino)cyclohexyl)amino)-[2,3'-bipyridin]-6-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years