化合物NVP-2

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 IC ₅₀ 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 IC ₅₀ 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.