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]
Enzyme inhibitor
This cyclin -directed inhibitor (FW = 345.34 g/mol; CAS 582315-72-8;
Solubility: 20 mg/mL DMSO; <1 mg/mL Water), also known systematically
as (4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl) (2,6-difluoro-4-methylphenyl)
methanone, targets CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM
and 9 nM, respectively. Cyclin Target Selectivity: Cdk1 (+++), Cdk2 (+++),
Cdk3 (weak, if any), Cdk4 (+), Cdk5 (weak, if any), Cdk6 (weak, if any),
Cdk7 (weak, if any), Cdk8 (weak, if any), Cdk9 (weak, if any), Cdk10
(weak, if any).
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.
