General description
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
Cell permeable: no
Primary Target
p34cdk1/cyclin B
Product competes with ATP.
Reversible: yes
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
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Physical form
A 50 mM (5 mg/282 µl) solution of Roscovitine (Cat. No. 557360) in DMSO.
Reconstitution
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
Meijer, L. 1996. Trends Cell Biol.6, 393.
Rudolph, B., et al. 1996. EMBO J.15, 3053.
Legal Information
Sold under license of U.S. Patent 6,316,456.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 354.45. Empirical Formula: C19H26N6O. Quality Level: 100. Assay: ≥. 95% (HPLC). form: liquid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, desiccated (hygroscopic), protect from light. shipped in: wet ice. storage temp.: 2-8°C. Storage Class Code: 10 - Combustible liquids. WGK: WGK 2. Flash Point(F): 188.6 °F - (Dimethylsulfoxide). Flash Point(C): 87 °C - (Dimethylsulfoxide).- UPC:
- 51171718
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 557364-5MG
