557364
Roscovitine
InSolution, ≥95%, inhibitor of cyclin-dependent kinases (CDKs)
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Synonym(s):
InSolution Roscovitine
Empirical Formula (Hill Notation):
C19H26N6O
Molecular Weight:
354.45
UNSPSC Code:
12352200
NACRES:
NA.77
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Quality Level
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
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
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.
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
WGK
WGK 2
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