GSK-3 Inhibitor XVI-CAS 252917-06-9-Calbiochem

C₂₂H₁₈Cl₂N₈

465.34

MFCD11846251

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). CHIR99021 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). CHIR99021 is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes models in vivo.
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. Also available as a 25 mM solution in DMSO (Cat. No. 361571).

Toxicity: Harmful (C)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

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.

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

200

≥97% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

light beige

DMSO: 5 mg/mL

ambient

2-8℃

5 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 3