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Description

A cell-permeable triaryl substituted imidazolo compound that acts as a potent, reversible and relatively specific ATP-competitive inhibitor of CK1 (IC50 = 0.2 µ,M from S. pombe, 0.3 µ,M for CK1delta) and ALK5 (IC50 = 0.5 µ,M). A weak inhibitor of p38alpha MAP kinase (IC50 = 12 µ,M) and only weakly affects the activities of a panel of kinases tested, including PKB, SGK and GSK-3beta. Suppresses the site-specific phosphorylation (Ser322 and Ser325) and nuclear exclusion of FOXO1a in H4IIE hepatoma cells. Shown to be ~10-fold more potent than IC261 (Cat. No. 400090, IC50 = 2.5 µ,M for CK1)., A cell-permeable, reversible, potent, and relatively specific ATP-competitive inhibitor of CK1 (IC50 = 200 nM from S. pombe, 0.3 µ,M for CK1delta) and ALK5 (IC50 = 500 nM). A weak inhibitor of p38alpha MAP kinase (IC50 = 12 µ,M) and several other kinases tested, including PKB, SGK, and GSK-3beta. Suppresses the site-specific phosphorylation (Ser322 and Ser325) and nuclear exclusion of FOXO1A in H4IIE hepatoma cells. Shown to be ~ 10-fold more potent than IC261 (Cat. No. 400090, IC50 = 2.5 µ,M for CK1).