A reversible, cell-permeable inhibitor of GSK3
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Isomer(s)
34872CHIR98024
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CHIR98014

Item No. 15578

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N6-[2-[[4-(2,4-dichlorophenyl)-5-(1H-imidazol-1-yl)-2-pyrimidinyl]amino]ethyl]-3-nitro-2,6-pyridinediamine
CAS Number
252935-94-7
Molecular Formula
C20H17Cl2N9O2
Formula Weight
486.3
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml
λmax
250, 315, 396 nm
SMILES
NC1=NC(NCCNC2=NC=C(N3C=CN=C3)C(C4=C(Cl)C=C(Cl)C=C4)=N2)=CC=C1[N+]([O-])=O
InChi Code
InChI=1S/C20H17Cl2N9O2/c21-12-1-2-13(14(22)9-12)18-16(30-8-7-24-11-30)10-27-20(29-18)26-6-5-25-17-4-3-15(31(32)33)19(23)28-17/h1-4,7-11H,5-6H2,(H3,23,25,28)(H,26,27,29)
InChi Key
MDZCSIDIPDZWKL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $90

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    5 mg

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    10 mg

    $349

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    25 mg

    $740

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    CHIR98014 is a reversible, cell-permeable inhibitor of GSK3α and GSK3β (IC50 = 0.65 and 0.58 nM, respectively).1 It is inactive against a series of other serine/threonine or tyrosine kinases.1 Through its effects on GSK3, CHIR98014 stimulates glycogen synthase in cells (EC50 = 106 nM), potentiates insulin-dependent glucose transport in isolated muscle strips, and improves glucose disposal in diabetic animals.1 CHIR98014 also reduces tau phosphorylation in rat brains and supports Wnt signaling during osteogenesis.2,3

    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. Selenica, M.L., Jensen, H.S., Larsen, A.K., et al. Efficacy of small-molecule glycogen synthase kinase-3 inhibitors in the postnatal rat model of tau hyperphosphorylation. Br J Pharmacol. Br. J. Pharmacol. 152(6), 959-979 (2007).

    3. Guerrero, F., Herencia, C., Almadén, Y., et al. TGF-β prevents phosphate-induced osteogenesis through inhibition of BMP and Wnt/β-catenin pathways. PLoS One 9(2), e89179 (2014).

    Product Citations

    Alavi, M.V. Tau phosphorylation and OPA1 proteolysis are unrelated events: Implications for Alzheimer’s Disease. Biochim. Biophys. Acta Mol. Cell Res. 1868(12), 119116 (2021).