Uses
BMS-265246 is a potent and selective pyra-zolopyridine based inhibitor of cdk2/cyclinE, cdk1/cyclinB and cdk4/ cyclinD.
Biological Activity
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]
IC 50
CDK1/cycB: 6 nM (IC
50); CDK2/Cyc E: 9 nM (IC
50); CDK4/cycD: 230 nM (IC
50)
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. bioorgmed 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.
