Roscovitine-CAS 186692-46-6-Calbiochem

C₁₉H₂₆N₆O

354.45

MFCD02266401

A potent, reversible, and selective inhibitor of cyclin-dependent kinases (Cdks) that exhibits about ten-fold greater efficacy towards p34^cdk1 and p33^cdk2 and twenty-fold greater efficacy towards p33^cdk5 relative to Olomoucine (Cat. No. 495620). Inhibits p34^cdk1/cyclin B (IC₅₀ = 650 nM), p33^cdk2/cyclin A (IC₅₀ = 700 nM), p33^cdk2/cyclin E (IC₅₀ = 700 nM), and p33^cdk5/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 p34^cdk4/cyclin D1 and p40^cdk6/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.

Primary Target
p34^cdk1/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

Toxicity: Standard Handling (A)

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

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.

Sold under license of U.S. Patent 6,316,456
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze

white to off-white

DMSO: 10 mg/mL

ambient

−20℃

1S/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

BTIHMVBBUGXLCJ-OAHLLOKOSA-N

1, 5 mg in Plastic ampoule

11 - Combustible Solids

WGK 3