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InSolution GSK-3 Inhibitor XVI, CHIR99021

InSolution GSK-3 Inhibitor XVI, CHIR99021, CAS 252917-06-9, is a 25 mM solution in DMSO. A cell-permeable, ATP-competitive inhibitor of GSK-3 (IC₅₀ = 10 & 6.7 nM for GSK-3α and GSK-3β, respectively).

InSolution GSK-3 Inhibitor XVI, CHIR99021, 6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile
Empirical Formula (Hill Notation):
CAS Number:
Molecular Weight:
MDL number:

Quality Level


≥95% (HPLC)





storage condition

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

shipped in


storage temp.




InChI key


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.

Biochem/physiol Actions

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


Packaged under inert gas


Toxicity: Irritant (B)

Physical form

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

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.

Legal Information

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

Storage Class Code

10 - Combustible liquids



Flash Point(F)

188.6 °F - (refers to pure substance)

Flash Point(C)

87 °C - (refers to pure substance)

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