(S)-CR8 是 CR8 的 S-异构体。 (S)-CR8 是一种有效的选择性 CDK 抑制剂，对 CDK2/cyclin E、CDK2/cyclin A、CDK9/cyclin T、CDK5/p25 和 CDK1/cyclin 的 IC50 分别为 0.060、0.080、0.11、0.12 和 0.15 μM B，分别。 (S)-CR8 降低 SH-SY5Y 细胞的存活率 (IC50 0.40 μM)。
货号:ajcx20960
CAS:1084893-56-0
分子式:C24H29N7O
分子量：431.5
溶解度:DMSO: soluble,Ethanol: soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

(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).¹It 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).²It 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)