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Cat. No. Name Size Price Add Cart
KI3320CHIR-98014QuoteQuote

Chemical Characteristic

Product NameCHIR-98014
CAS No.252935-94-7
Molecular Weight 486.31
FormulaC20H17Cl2N9O2
Chemical NameN2-(2-(4-(2,4-dichlorophenyl)-5-(1H-imidazol-1-yl)pyrimidin-2-ylamino)ethyl)-5-nitropyridine-2,6-diamine
Smilesc1(c(ccc(n1)NCCNc1nc(c(cn1)n1cncc1)c1c(cc(cc1)Cl)Cl)[N](=O)O)N
Chemical Structure

Biological activities

CHIR-98014 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3). The IC50s of CHIR-98014 against human GSK-3α and GSK-3β is 0.65 and 0.58 nM, respectively. CHIR-98014 inhibits human GSK-3β with a Ki of 0.87 nM. The EC50s of CHIR-98014 for glycogen synthase (GS) in CHO-IR cells and rat hepatocytes are 106 and 107 nM, respectively.[1] Acute treatment (30 minutes) of CHIR-98014 does-dependently activates GS in cultured human skeletal muscle cells with a maximally effective concentration of approximately 2 µM.[2] CHIR-98014 increases the sensitivity of soleus muscle from ZDF rats to insulin, increasing the maximal rate of glucose transport to 71% of the rate in muscle from lean animals. In diabetic and insulin-resistantdb/db mice in vivo, CHIR-98014 treatment (30 mg/kg) within 4 hours displays a significant reduction in fasting hyperglycemia and shows improved glucose disposal during an (intraperitoneal glucose tolerance test) ipGTT.[1] Furthermore, CHIR-98014 also decreases tau phosphorylation (Ser396) in the cortex and hippocampus of postnatal rats in vivo.[3]

Protocols

In vitro: CHIR-98014 is dissolved in DMSO.[3]

References

[1] Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003, 52(3): 588-595.
[2] Nikoulina SE, et al. Inhibition of glycogen synthase kinase 3 improves insulin action and glucose metabolism in human skeletal muscle. Diabetes. 2002, 51(7): 2190-2198.
[3] Selenica ML, et al. Efficacy of small-molecule glycogen synthase kinase-3 inhibitors in the postnatal rat model of tau hyperphosphorylation. Br J Pharmacol. 2007, 152(6): 959-979.

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