Roscovitine-CAS 186692-46-6-Calbiochem

半岛bd体育手机客户端 说明

一般描述

A potent, reversible, and selective inhibitor of cyclin-dependent kinases (Cdks) that exhibits about ten-fold greater efficacy towards p34^cdk1and p33^cdk2and twenty-fold greater efficacy towards p33^cdk5relative to Olomoucine (Cat. No. 495620). Inhibits p34^cdk1/cyclin B (IC₅₀= 650 nM), p33^cdk2/cyclin A (IC₅₀= 700 nM), p33^cdk2/cyclin E (IC₅₀= 700 nM), and p33^cdk5/p35 (IC₅₀= 200 nM) by competing for the ATP binding domain of the kinases. Exhibits reduced sensitivity towards related kinases including ERK1 and ERK2 (IC₅₀= 34 ?M and 14 ?M, respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100 ?M, including p34^cdk4/cyclin D1 and p40^cdk6/cyclin D2. Compared to olomoucine, roscovitine displays increased anti-mitotic activity at the G₁/S and G₂/M phases of the cell cycle. A 50 mM (5 mg/282 ?l) solution of Roscovitine (Cat. No. 557364) in DMSO is also available.
A potent, reversible, and selective inhibitor of cyclin-dependent kinases (cdks). Exhibits greater inhibitory potency compared to olomoucine (Cat. No. 495620). Inhibits p34^cdc2/cyclin B (IC₅₀= 0.65 ?M), p33^cdk2/cyclin A (IC₅₀= 0.70 ?M), p33^cdk2/cyclin E (IC₅₀= 0.70 ?M), and p33^cdk5/p35 (IC₅₀= 0.20 ?M) by competing for the ATP binding domain of these kinases. Exhibits very low sensitivity towards related kinases, such as erk1 and erk2 (IC₅₀= 34 ?M and 14 ?M, respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100 ?M and compared to olomoucine, roscovitine displays increased anti-mitotic activity at the G1/S and G2/M phases of the cell cycle.

包装

1, 5 mg in Plastic ampoule

生化/生理作用

Primary Target
p34^cdk1/cyclin B
Product does not compete with ATP.
Target IC₅₀: 650 nM, 700 nM, 700 nM, 200 nM, against p34cdk1/cyclin B, p33cdk2/cyclin A, p33cdk2/cyclin E, p33cdk5/p35, respectively
Cell permeable: no
Reversible: yes

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for at least 6 months at -20°C.

其他说明

De Azevedo, W.F., et al. 1997.Eur. J. Biochem.243,518.
Meijer, L., et al. 1997.Eur. J. Biochem.243,527.
Meijer, L., et al. 1996.Trends Cell Biol.6,393.
Rudolph, B., et al. 1996.EMBO J.15,3053.

法律信息

Sold under license of U.S. Patent 6,316,456
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式	C19H26N6O
分子量	354.45
MDL编号	MFCD02266401

半岛bd体育手机客户端 性质

质量水平	100
测定	≥95% (HPLC)
形式	solid
manufacturer/tradename	Calbiochem?
储存条件	OK to freeze
颜色	white to off-white
溶解性	DMSO: 10 mg/mL
运输	ambient
储存温度	?20℃
InChI	1S/C19H26N6O/c1-4-15(11-26)22-19-23-17(20-10-14-8-6-5-7-9-14)16-18(24-19)25(12-21-16)13(2)3/h5-9,12-13,15,26H,4,10-11H2,1-3H3,(H2,20,22,23,24)/t15-/m1/s1
InChI key	BTIHMVBBUGXLCJ-OAHLLOKOSA-N

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable