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

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一般描述

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 ?M against 20 kinases and K_i≥5 ?M against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (K_d~4 ?M). CHIR99021 is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes modelsin 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 ?M against 20 kinases and K_i≥5 ?M against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (K_d~4 ?M). This compound is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes modelsin vivo. Also available as a 25 mM solution in DMSO (Cat. No. 361571).

包装

5 mg in Plastic ampoule
Packaged under inert gas

警告

Toxicity: Harmful (C)

重悬

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

其他说明

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.

法律信息

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

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