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 Ki ≥5 µM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (Kd ~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)
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