Stemolecule™ CHIR99021

The aminopyrimidine CHIR99021 is the most selective inhibitor of glycogen synthase kinase 3 β (GSK-3β) reported to date^1,2. Unlike other potent inhibitors of GSK-3, CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs³. Along with the elimination of differentiation-inducing signaling from mitogen-activated protein kinases, using CHIR99021 to block the activity of GSK-3β enables the self-renewal of embryonic stem cells⁴.

Stemolecule CHIR99021 is also available as a 10 mM DMSO Stock Solution in DMSO (2 mg in 429.8 μl) (Cat. No. 04-0004-02).

Stemgent and the Stemolecule brand name are trademarks of REPROCELL Inc., Japan.

Product Name: Stemolecule CHIR99021

Catalog Number: 04-0004

Size:

• 2 mg (Cat. No. 04-0004)
• 10 mg (Cat. No. 04-0004-10)
• 2 mg in 10 mM DMSO solution  (2 mg in 429.8 μl) (Cat. No. 04-0004-02)

Alternate Name(s): 6-[[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2 pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile

Chemical Formula: C₂₂H₁₈Cl₂N₈

Molecular Weight: 465.34

CAS Number: 252917-06-9

Purity: Greater than 95 % by HPLC analysis

Formulation: Off-white solid

Solubility: Reconstitute in DMSO to the desired concentration. For reconstitution instructions please reference product specifications sheet.

Storage and Stability: Store powder at 4 °C protected from light. Information about the stability of Stemolecules in solution is largely not available. As a general guideline, we recommend that stock solution be freshly made and stored in aliquots at −20 °C. The effect of storage of stock solutions should be verified for each application.

Quality Control: The purity of CHIR99021 was determined by HPLC analysis. The accurate mass was determined by mass spectrometry. Cellular toxicity of CHIR99021 was tested on mouse embryonic stem cells.

Specification Sheets:

• 04-0004 Specifications Sheet
• 04-0004-10 Specifications Sheet
• 04-0004-02 Specifications Sheet

Safety Data Sheets:

• 04-0004 and 04-0004-10 Safety Data Sheet
• 04-0004-02 Safety Data Sheet

1. Sato, N., Meijer, L., Skaltsounis, L., Greengard, P., and Brivanlou, A.H. Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor. Nat Med 10: 55-63 (2004).
2. Besser, D. (2004) Expression of nodal, lefty-a, and lefty-B in undifferentiated human embryonic stem cells requires activation of Smad 2/3. J Biol Chem 279: 45076-45084 (2004).
3. Ying, Q.L., Wray, J., Nichols, J., Batlle-Morera, L., Doble, B., Woodgett, J., Cohen, P., and Smith, A. The ground state of embryonic stem cell self renewal. Nature 453: 519-523 (2008).
4. Polychronopoulos, P., Magiatis, P., Skaltsounis, A.L., Myrianthopoulos, V., Mikros, E., Tarricone, A., Musacchio, A., Roe, S.M., Pearl, L., Leost, M., Greengard, P., and Meijer, L. Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. J Med Chem 47: 935-946 (2004).

Additional Publications

• Karami N; Taei A; Hassani SN; Alizadeh N; Eftekhari-Yazdi P; Hassani F. The effects of insulin–transferrin–selenium (ITS) and CHIR99021 on the development of pre-implantation human arrested embryos in vitro. Sci Rep 15:5006 (2025).
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• Gulieva RE; Ahmadvand P; Freedman BS. A novel rapalog shows improved safety vs. efficacy in a human organoid model of polycystic kidney disease. Stem Cell Reports 20:102395 (2025).
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