CHIR98014

The two isoforms of glycogen synthase kinase 3, GSK3alpha and GSK3beta, constitutively phosphorylates and inactivates glycogen synthase, preventing glycogen synthesis. They also phosphorylate proteins that are relevant to Alzheimer's disease and osteogenesis. CHIR98014 is a reversible, cell-permeable inhibitor of GSK3alpha and GSK3beta (IC50 = 0.65 and 0.58 nM, respectively). It is inactive against a series of other serine/threonine or tyrosine kinases. 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. CHIR98014 also reduces tau phosphorylation in rat brains and supports Wnt signaling during osteogenesis.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: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml. lambdamax: 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.