BMS265246 is a potent and selective inhibitor for CDK1 and CDK2 (IC50= 6 nM and 9 nM)
Cyclin-dependent kinases (CDK) are a group of serine/threonine kinases. They are activated by coupling to cyclin and participate in the regulation of cell cycle.
BMS265246 inhibited the Cdk4/cycD activity and prevented A2780 Cytox (IC50 = 0.23 μM and 0.76 μM) [1]. In HCT-116 cells, BMS-265246 blocked the cell proliferation (EC50= 0.293 μm—0.492 μm). Following the treatment of BMS-265246, low DNA intensity, large round nuclei and 4N DNA content were observed in the dominant cell population –G2 arrested cells. [2]
References:
1. Misra RN, Xiao Hy, Rawlins DB et al. 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg
Med Chem Lett. 2003 Jul 21;13(14):2405-8.
2. Sutherland JJ, Low J, Blosser W et al. A robust high-content imaging approach for probing the mechanism of action and phenotypic outcomes of cell-cycle modulators. Mol Cancer Ther. 2011 Feb;10(2):242-54.