Soluble in DMSO (10 mg/ml), water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25 °C., Soluble in DMSO (10 mg/ml), water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25 °C.
A compound that acts as potent, ATP-competitive & highly selective GSK-3 inhibitor
生化機(jī)理
GSK-3 Inhibitor XVI is 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 Ki ≥5 μM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (Kd ~4 μM).