Biochem/physiol Actions

Reversible: yes

Target IC₅₀: 10 and 6.7 nM against GSK-3&alpha

Primary TargetGSK-3 α and β

Cell permeable: yes

General description

A cell-permeable aminopyrimidine compound that acts as potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC₅₀ = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively). Exhibits little or no activity toward 46 other enzymes (IC₅₀ >8.8 µM against 20 kinases and K_i ≥5 µM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (K_d ~4 µM). This compound is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes models in vivo. The solid form of this compound (Cat. No. 361559) is also available.

Legal Information

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

Other Notes

Mussmann, R., et al. 2007. J. Biol. Chem.282, 12030. Ring, D.B., et al. 2003. Diabetes52, 588.Bennett, C.N., et al. 2002. J. Biol. Chem.277, 30998.Cline, G.W., et al. 2002. Diabetes51, 2903.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Physical form

A 25 mM (5 mg/430 µL) solution of GSK-3 Inhibitor XVI, CHIR99021 (Cat. No. 361559) in DMSO.

Warning

Toxicity: Irritant (B)