现货,Roscovitine (Seliciclib),CAS号:186692-46-6,美国进口,细胞周期(Cell Cycle / Checkpoint),CDK , CDK 抑制剂和化合物

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> CDK >> CDK 抑制剂和化合物 >> Roscovitine (Seliciclib)http://selleck.cn/roscovitine-S1153.html

技术数据:

分子量(MW): 354.45

化学式:

C19H26N6O

 

溶解度: DMSO ≥71mg/mL Water <1mg/mL Ethanol ≥71mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 186692-46-6

生物活性

 

 

Roscovitine (Seliciclib) is a potent and selective inhibitor of cyclin-dependent kinases (cdks). This agent displays higher inhibitory potency and higher selectivity compared to olomoucine. [1]

Roscovitine inhibits p34 cdc2/cyclin B (IC50 = 0.65 µM), p33 cdk2/cyclin A(IC50 = 0.70 µM), p33 cdk2/cyclin E (IC50 = 0.70 µM), and p33 cdk2/p35(IC50 = 0.20 µM) by competing for the ATP binding domain of these kinases. Roscovitine exhibits very low sensitivity towards related kinases, such as erk1 and erk2 (IC50 = 34 µM and 14 µM, respectively) .[2]

Roscovitine doesnot significantly affect the activity of other protein kinases even at 100 µM and compared to olomoucine. Roscovitine displays increased anti-mitotic activity at the G1/S and G2/M phases of the cell cycle. [3]

 

 

 

参考文献

Inhibition of cyclin-dependent kinases by purine analogues Crystal structure of human cdk2 complexed with roscovitine Walter Filgueira DE AZEVEDO,Sophie LECLERC,et al. Eur. J. Biochem 1997;243:518-526

Roscovitine, a novel cyclin-dependent kinase inhibitor, characterizes restriction point and G2/M transition in tobacco BY-2 cell suspension S6verine Planchais,Nathalie Glab,et al. The Plant Journal 1997;12(1), 191-202

Roscovitine inhibits the proliferative activity of immortal and neoplastic human breast epithelial cells. Mgbonyebi OP, Russo J, Russo IH. Anticancer Res. 1998 Mar-Apr;18(2A):751-5.

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