CHIR-98014 is a potent, selective glycogen synthase kinase 3 (GSK-3) withIC50 of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively.
CHIR-98014 shows less potent activities against 20 other protein kinases including Cdc2 and Erk2; causes GS stimulation in CHO-IR cells and rat hepatocytes, with EC50s of 106 nM and 107 nM, respectively.
CHIR-98014 reduces the viability of ES-CCE cells with IC50 of 1.1 uM, results in a significant activation of the Wnt/beta-catenin pathway in ES-D3 cells combined with CHIR-99021.
CHIR-98014 significantly reduces fasting hyperglycemia within and shows improved glucose disposal in diabetic and insulin-resistant db/db mice.
