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Roscovitine-CAS 186692-46-6-Calbiochem

品牌
Sigma-Aldrich
CAS
186692-46-6
货号
557360
规格纯度
A potent, reversible, and selective inhibitor of Cdks that exhibits about 10-fold greater efficacy towards p34-cdk1 and p33-cdk2 and 20-fold greater efficacy towards p33-cdk5 relative to Olomoucine.
参考价格
941.52 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

A potent, reversible, and selective inhibitor of cyclin-dependent kinases (Cdks) that exhibits about ten-fold greater efficacy towards p34cdk1 and p33cdk2 and twenty-fold greater efficacy towards p33cdk5 relative to Olomoucine (Cat. No. 495620). Inhibits p34cdk1/cyclin B (IC50 = 650 nM), p33cdk2/cyclin A (IC50 = 700 nM), p33cdk2/cyclin E (IC50 = 700 nM), and p33cdk5/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 µM and 14 µM, respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100 µM, including p34cdk4/cyclin D1 and p40cdk6/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 µl) 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 µM), p33 cdk2/cyclin A (IC50 = 0.70 µM), p33 cdk2/cyclin E (IC50 = 0.70 µM), and p33 cdk5/p35 (IC50 = 0.20 µM) by competing for the ATP binding domain of these kinases. Exhibits very low sensitivity towards related kinases, such as erk1 and erk2 (IC50 = 34 µM and 14 µM, respectively). Roscovitine does not 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.

包装

1, 5 mg in Plastic ampoule

生化/生理作用

Primary Target
p34cdk1/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

产品性质

质量水平100
测定≥95% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
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℃
InChI1S/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 keyBTIHMVBBUGXLCJ-OAHLLOKOSA-N

安全信息

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

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