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CHIR98014
- CT98014
- Moderately soluble in DMSO
- MF: C20H17Cl2N9O2
- MW: 486.31
Description
CHIR98014 is a highly potent, selective, cell-permeable and reversible glycogen synthase kinase-3 (GSK-3) inhibitor with IC₅₀ values of 0.65 nM (GSK-3α) and 0.58 nM (GSK-3β) and >500-fold selectivity for GSK-3 over more than 20 other kinases. It is a recommended tool compound for studies of GSK-3-dependent signaling and widely used in cell signaling and stem cell research as an activator of the Wnt/β-catenin pathway.
GSK-3 regulates Wnt/β-catenin signaling, glycogen metabolism, neuronal biology, inflammation and cell fate decisions. CHIR98014 is useful for probing GSK-3α/β activity in biochemical and cell-based models.
Key Features
- Very potent GSK-3 inhibitor
- Selective, cell-permeable and reversible
- Useful for GSK-3α/β pathway studies
- Recommended research tool for kinase signaling
Applications
- GSK-3 inhibition assays
- Wnt/β-catenin signaling research
- Stem cell and differentiation studies
- Metabolic and neurobiology pathway models
More Information
| Parent CAS No. | 252935-94-7 |
|---|---|
| Chemical Name | N*6*-{2-[4-(2,4-Dichloro-phenyl)-5-imidazol-1-yl-pyrimidin-2-ylamino]-ethyl}-3-nitro-pyridine-2,6-diamine |
| SMILES | C1(NCCNC2N=C(C3C(Cl)=CC(Cl)=CC=3)C(N3C=NC=C3)=CN=2)N=C(N)C([N+]([O-])=O)=CC=1 |
| MFCD | MFCD10565922 |
| InChi | 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) |
| InChiKey | MDZCSIDIPDZWKL-UHFFFAOYSA-N |
| CID | 53396311 |
| Short Description | GSK-3 inhibitor |
References
- ML Selenica et al. Efficacy of small-molecule glycogen synthase kinase-3 inhibitors in the postnatal rat model of tau hyperphosphorylation. Br. J. Pharmacol. 2007, 152, 959–979.
- SE Nikoulina et al. Inhibition of Glycogen Synthase Kinase 3 Improves Insulin Action and Glucose Metabolism in Human Skeletal Muscle. Diabetes 2002, 51(7), 2190-2198.
- DB Ring et al. Selective glycogen synthase kinase inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes 2003, 52, 588–595.
- AS Wagman et al. Discovery and development of GSK3 inhibitors for the treatment of type 2 diabetes. Curr. Pharm. Des. 2004, 10, 1105–1137.
- List of publications using CHIR 98014 (Axon 1126) purchased from Axon Medchem
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