InSolution GSK-3 Inhibitor XVI, CHIR99021-CAS 252917-06-9-Calbiochem

产品说明

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). 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.

包装

5 mg in Glass bottle
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Primary Target
GSK-3 α and β
Reversible: yes
Target IC₅₀: 10 and 6.7 nM against GSK-3&alpha

警告

Toxicity: Irritant (B)

外形

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

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

基本信息

产品性质

安全信息