An inhibitor of cyclin-dependent kinases
(S)-CR8 is a second generation derivative of (R)-roscovitine and an inhibitor of cyclin-dependent kinase 1 (Cdk1/cyclin B), Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk9/cyclin T (IC50s = 0.15, 0.08, 0.06, 0.12, and 0.11 µM, respectively).1 It also inhibits casein kinase CK1δ/ε (CKδ/ε) and DYRK1A (IC50s = 0.61 and 0.9 µM, respectively). (S)-CR8 reduces cell viability in human neuroblastoma cell lines, including SH-SY5Y, SK-N-AS, SK-N-BE, and IMR32 cells (IC50s = 0.43, 1.46, 0.13, and 0.14 µM, respectively).2 It also reduces protein levels of the survival factor Mcl-1 in SH-SY5Y cells.
1.Bettayeb, K., Oumata, N., Echalier, A., et al.CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinasesOncogene27(44)5797-5807(2008) 2.Bettayeb, K., Baunbaek, D., Delehouze, C., et al.CDK inhibitors roscovitine and CR8 trigger Mcl-I down-regulation and apoptotic cell death in neuroblastoma cellsGenes Cancer1(4)369-380(2010)
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