A selective GSK3 inhibitor
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CHIR99021

Item No. 13122

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile
CAS Number
252917-06-9
Synonyms
  • CT 99021
  • Laduviglusib
Molecular Formula
C22H18Cl2N8
Formula Weight
465.3
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 2.5 mg/ml
λmax
279 nm
SMILES
N#CC(C=N1)=CC=C1NCCNC2=NC=C(C3=NC(C)=CN3)C(C4=CC=C(Cl)C=C4Cl)=N2
InChi Code
InChI=1S/C22H18Cl2N8/c1-13-10-29-21(31-13)17-12-30-22(32-20(17)16-4-3-15(23)8-18(16)24)27-7-6-26-19-5-2-14(9-25)11-28-19/h2-5,8,10-12H,6-7H2,1H3,(H,26,28)(H,29,31)(H,27,30,32)
InChi Key
AQGNHMOJWBZFQQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $42

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    5 mg

    $126

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    10 mg

    $210

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    25 mg

    $473

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    Cayman Chemical
    Explore Obesity & Metabolic Disease Resources

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    OBESITY RESEARCH SOLUTIONS
    Product Description

    CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively.1 When tested against twenty different protein kinases, this inhibitor shows greater than 500-fold selectivity for GSK3. CHIR99021 activates glycogen synthesis in CHO-IR cells (EC50 = 0.763 μM) and in isolated type 1 diabetic rat skeletal muscle. A single oral dose (30 mg/kg) of CHIR99021 enhances in vivo glucose metabolism in a rodent model of type 2 diabetes. CHIR99021 has also been shown to induce the reprogramming of murine and human somatic cells into stem cells.2,3 This product is also available as part of Cayman's Astrocyte Reprogramming Reagent Kit (DFICBY) (Item No. 502887), Stem Cell Expansion Reagent Kit (SCB) (Item No. 502886), Hepatocyte Differentiation Reagent Kit (Item No. 44737).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ring, D.B., Johnson, K.W., Henriksen, E.J., et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes 52(3), 588-595 (2003).

    2. Li, W., Zhou, H., Abujarour, R., et al. Generation of human-induced pluripotent stem cells in the absence of exogenous Sox2. Stem Cells 27(12), 2992-3000 (2009).

    3. Ying, Q.L., Wray, J., Nichols, J., et al. The ground state of embryonic stem cell self-renewal. Nature 453(7194), 519-524 (2008).

    Product Citations

    Yeh, H., De Cruz, M.A., You, Y., et al. Development and characterization of in vitro inducible immortalization of a murine microglia cell line for high throughput studies. Sci. Rep. 15(1), 3207 (2025).

    Sorge, M., Savoré, G., Gallo, A., et al. An intrinsic mechanism of metabolic tuning promotes cardiac resilience to stress. EMBO Mol. Med. 16(10), 2450-2484 (2024).

    Hoes, M.F., Grote Beverborg, N., Kijlstra, J.D., et al. Iron deficiency impairs contractility of human cardiomyocytes through decreased mitochondrial function. Eur. J. Heart Fail. 20(5), 910-919 (2018).

    Wang, Q., Geng, Z., Gong, Y., et al. WDR68 is essential for the transcriptional activation of the PRC1-AUTS2 complex and neuronal differentiation of mouse embryonic stem cells. Stem Cell Res. 33, 206-214 (2018).