NVP-2

• CAT Number: I020454
• CAS Number: 1263373-43-8
• Molecular Formula: C₂₇H₃₇ClN₆O₂
• Molecular Weight: 513.07
• Purity: ≥95%

NVP-2 (CAT: I020454) is a potent and selective ATP-competitive inhibitor of cyclin-dependent kinase 9 (CDK9), with an IC50 of 0.514 nM. It also exhibits inhibitory effects on CDK1/CycB, CDK2/CycA, and CDK16/CycY kinases. NVP-2 has shown anti-proliferative activity in leukemia cells, with varying IC50 values across different cell lines. It induces cell apoptosis and engages CDK9 in both wildtype and CRBN−/− MOLT4 cells. Additionally, NVP-2 exhibits CRBN-dependent anti-proliferative and pro-apoptotic effects in MOLT4 cells. Treatment with NVP-2 induces cell apoptosis and upregulates caspase-3 and γH2A.X expression. These findings suggest the potential of NVP-2 as a therapeutic agent for leukemia and highlight its selective inhibition of CDK9 activity.

Reference

[1]. Winter GE, et al. BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment.Mol Cell. 2017 Jul 6;67(1):5-18.e19.