InSolutionTM GSK-3 Inhibitor XVI; CHIR99021

Code: 361571-5MG D2-231

Biochem/physiol Actions

Reversible: yes

Target IC50: 10 and 6.7 nM against GSK-3&alpha

Primary TargetGSK-3 α and β

Cell permeable: yes<...


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€348.40 EACH
Discontinued
€428.53 inc. VAT

Biochem/physiol Actions

Reversible: yes

Target IC50: 10 and 6.7 nM against GSK-3&alpha

Primary TargetGSK-3 α and β

Cell permeable: yes

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.

Legal Information

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

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.

Packaging

5 mg in Glass bottle

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.

Warning

Toxicity: Irritant (B)

assay≥95% (HPLC)
formliquid
manufacturer/tradenameCalbiochem®
Quality Level100
shipped inambient
storage conditiondesiccated (hygroscopic), avoid repeated freeze/thaw cycles, protect from light, OK to freeze
storage temp.−70°C
Cas Number252917-06-9
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