Biochem/physiol Actions

Cell permeable: no

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 0.6 µM and 0.4 µM for Cdk1/cyclin B and Cdk5/p25, respectively

Primary TargetCdk1/cyclin B, Cdk5/p25

General description

A 3-amino substituted pyrazoloquinoxaline compound that acts as a selective inhibitor of cyclin-dependent kinases 1 and 5 (Cdks; IC₅₀ = 0.6 µM and 0.4 µM for Cdk1/cyclin B and Cdk5/p25, respectively). Also shown to inhibit GSK-3β with (IC₅₀ = 1 µM). Does not inhibit Cdc25 phosphatase activity (IC₅₀ >10 µM).

A selective inhibitor of cyclin-dependent kinases 1 and 5 (Cdk1/Cdk5) (IC₅₀ = 600 nM for Cdk1/cyclin B and 400 nM for Cdk5/p25). Also shown to inhibit glycogen synthase kinase-3β (GSK-3β) (IC₅₀ = 1 µM). Does not inhibit Cdc25 phosphatase activity (IC₅₀ >10 µM).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Ortega, M.A., et al. 2002. Bioorg. Med. Chem.10, 2177.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)