产品简称

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.

溶解度

DMSO: 10 mg/mL

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.

一般描述

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.

生化/生理作用

Target IC₅₀: 650 nM, 700 nM, 700 nM, 200 nM, against p34cdk1/cyclin B, p33cdk2/cyclin A, p33cdk2/cyclin E, p33cdk5/p35, respectively

重悬

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

警告

Toxicity: Standard Handling (A)

法律信息

Sold under license of U.S. Patent 6,316,456