NVP-2 is an effective and selective ATP-competitive cyclin-dependent kinase 9 (CDK9) probe. NVP-2 induces cell apoptosis. NVP-2 inhibits CDK9/CycT activity (IC50: 0.514 nM). NVP-2 shows inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases (IC50: 0.584 μM, 0.706 μM, and 0.605 μM, respectively).

CDK9:0.5 nM (IC50)

NVP-2 has an anti-proliferation of leukemia cells, suppresses 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 (0-10 nM; 72 hours) shows CRBN-dependent anti-proliferative and pro-apoptotic effects in MOLT4 cells (IC50: 9 nM). NVP-2 (250 nM; 24 hours) causes 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. 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.