InSolution GSK-3 Inhibitor XVI, CHIR99021-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). 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.

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

Toxicity: Irritant (B)

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

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

100

≥95% (HPLC)

liquid

Calbiochem^®

OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light

ambient

−70℃

5 mg in Glass bottle
Packaged under inert gas

10 - Combustible liquids

WGK 2

188.6 °F - (refers to pure substance)

87 ℃ - (refers to pure substance)