Merck, 361571-5MG, GSK-3 Inhibitor XVI, CHIR99021

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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
GSK-3 α and β
Reversible: yes
Target IC₅₀: 10 and 6.7 nM against GSK-3&alpha
Packaging
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)