Biochem/physiol Actions

Cell permeable: no

Reversible: no

Target IC₅₀: 10 nM against GSK-3α/β

Product does not compete with ATP.

Primary TargetGSK-3α/β

General description

An acetoxime analog of BIO, GSK-3 Inhibitor IX (Cat. No. 361550) that exhibits greater selectivity for GSK-3α/β (IC₅₀ = 10 nM) over Cdk5/p25, Cdk2/cyclin A, and Cdk1/cyclin B (IC₅₀ = 2.4 µM, 4.3 µM, and 63 µM, respectively). A weak inhibitor of Cdk4/cyclin D1 and many other non-related kinases (IC₅₀ ≥ 10 µM). Yields BIO (Cat. No. 361550) upon hydrolysis.

An acetoxime analog of BIO, GSK-3 Inhibitor IX (Cat. No. 361550) that exhibits greater selectivity for GSK-3α/β (IC₅₀ = 10 nM) over Cdk5/p25, Cdk2/A and Cdk1/B (IC₅₀ = 2.4 µM, 4.3 µM and 63 µM, respectively). Weakly affects the activities of Cdk4/D1 and many other kinases (IC₅₀ ≥ 10 µM). Also acts as an aryl hydrocarbon receptor agonist in both yeast (EC₅₀ ≥ 0.1 µM) and mammalian (EC₅₀ = 0.16 µM) reporter systems.

Legal Information

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

Other Notes

Knockaert, M., et al. 2004. Oncogene23, 4400.Polychronopoulos, P., et al. 2004. J. Med. Chem.47, 935.Meijer, L., et al. 2003. Chem. Biol.10, 1255.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Preparation Note

Limited solubility in aqueous buffers; serial dilutions in DMSO may be required prior to dilution in buffer.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Carcinogenic / Teratogenic (D)