A cell-permeable aminopyrimidine compound that acts as potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC50 = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively). CHIR99021 exhibits little to no activity toward 46 other enzymes (IC50>8.8 µM against 20 kinases and Kι ≥5 µM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (Kd ~4 µM). CHIR99021 is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes models in vivo.
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CL1006 Laduviglusib(CHIR 99021;CT 99021) (252917-06-9)