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基本信息
Empirical Formula【经验(实验)分子式】 | C19H26N6O |
Molecular weight | 354.45 |
General description【一般描述】 | A potent and selective inhibitor of cyclin-dependent kinases (Cdks). Exhibits greater inhibitory potency compared to olomoucine (Cat. No. 495620). Inhibits p34 Cdc2/cyclin B (IC50 = 650 nM), p33 Cdk2/cyclin A (IC50 = 700 nM), p33 Cdk2/cyclin E (IC50 = 700 nM), and p33 Cdk2/p35 (IC50 = 200 nM) 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. |
Biochem/physiol Actions【生化/生理作用】 | Reversible: yes Primary Target p34cdk1/cyclin B Product competes with ATP. Target IC50: 650 nM, 700 nM, 700 nM, and 200 nM against p34cdk1/cyclin B, p33cdk2/cyclin A, p33cdk2/cyclin E, and p33cdk5/p35, respectively Cell permeable: no |
Warning【警告】 | Toxicity: Irritant (B) |
Physical form【外形】 | A 50 mM (5 mg/282 µl) solution of Roscovitine (Cat. No. 557360) in DMSO. |
Reconstitution【重悬】 | Following initial use, aliquot and freeze (-20°C). Once opened, the DMSO aliquots are stable for up to 6 months at -20°C. |
Other Notes【其他说明】 | Meijer, L. 1996. Trends Cell Biol.6, 393. Rudolph, B., et al. 1996. EMBO J.15, 3053. |
Legal Information【法律信息】 | Sold under license of U.S. Patent 6,316,456. CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥95% (HPLC) |
form【形式】 | liquid |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze desiccated (hygroscopic) protect from light |
shipped in【运输】 | wet ice |
storage temp.【储存温度】 | 2-8℃ |
packaging【包装】 | 5 mg in Plastic ampoule Packaged under inert gas |
安全信息
Storage Class Code【储存分类代码】 | 10 - Combustible liquids |
WGK | WGK 2 |
Flash Point(F)【闪点(F)】 | 188.6 °F - (Dimethylsulfoxide) |
Flash Point(C)【闪点(C)】 | 87 ℃ - (Dimethylsulfoxide) |