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 hours |
Result: |
Degrade CDK9 sub-stoichiometrically at all concentrations. |
Apoptosis Analysis
Cell Line: |
Wildtype and CRBN MOLT4 cells |
Concentration: |
250 nM |
Incubation Time: |
24 hours |
Result: |
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 in MOLT4 cells. |