NVP-2,1263373-43-8

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NVP-2

CAS No. : 1263373-43-8

MCE 国际站：NVP-2

产品活性：NVP-2 是一种有效且具有选择性的 ATP 竞争性细胞周期蛋白依赖性激酶 9 (CDK9) 探针，可抑制 CDK9/CycT 活性，IC₅₀ 值为 0.514 nM。NVP-2 对 CDK1/CycB，CDK2/CycA 和 CDK16/CycY 激酶具有抑制作用，其 IC₅₀ 值分别为 0.584 µM，0.706 µM 和 0.605 µM。NVP-2诱导细胞凋亡 (apoptosis)。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：CDK  |  Apoptosis

In Vitro: 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.

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