Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Target IC₅₀: 230 nM, 470 nM, 400 nM, 680 nM, 7.5 µM, 850 nM, 15 µM, 20 µM, 20 µM, 9 µM against glycogen synthase kinase-3β, Lck IC50, Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, c-Src, casein kinase II, ERK1, and ERK2

Cell permeable: yes

General description

A potent cell-permeable and reversible inhibitor of glycogen synthase kinase-3β (IC₅₀ = 230 nM), Lck (IC₅₀ = 470 nM), and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC₅₀ = 400 nM), Cdk2/cyclin A (IC₅₀ = 680 nM), Cdk2/cyclin E (IC₅₀ = 7.5 µM), and Cdk5/p25 (IC₅₀ = 850 nM). Also inhibits other kinases such as c-Src (IC₅₀ = 15 µM), casein kinase II (IC₅₀ = 20 µM), ERK1 (IC₅₀ = 20 µM), and ERK2 (IC₅₀ = 9 µM). Inhibition is competitive with respect to ATP binding.

A potent, cell-permeable, and reversible inhibitor of glycogen synthase kinase-3β (IC₅₀ = 230 nM), Lck (IC₅₀ = 470 nM), and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC₅₀ = 400 nM), Cdk2/cyclin A (IC₅₀ = 680 nM), Cdk2/cyclin E (IC₅₀ = 7.5 µM), and Cdk5/p25 (IC₅₀ = 850 nM). Also inhibits other kinases such as c-Src (IC₅₀ = 15 µM), casein kinase II (IC₅₀ = 20 µM), ERK1 (IC₅₀ = 20 µM), and ERK2 (IC₅₀ = 9 µM). Inhibition is competitive with respect to ATP binding.

Legal Information

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

Other Notes

Bain, J., et al. 2003. Biochem. J. 371, 199.Buolamwini, J.K. 2000. Curr. Pharm. Des.6, 379.Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.Zaharevitz, D.W., et al. 1999. Cancer Res. 59, 2566.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)