CK1 Inhibitor 4-(4-(2,3-Dihydrobenzo[1,4]dioxin-6-yl)-5-pyridin-2-yl-1H-imidazol-2-yl)benzamide Light yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable triaryl substituted imidazolo compound that acts as a potent and relatively specific ATP-competitive inhibitor of CK1 (IC50 = 0.2 µM from S. pombe; 0.3 µM for CK1d) and ALK5 (IC50 = 0.5 µM). A weak inhibitor of p38a MAP kinase (IC50 = 12 µM) and only weakly affects the activities of a panel of kinases tested, including PKB, SGK and GSK-3b. 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 µM for CK1). Purity: ≥95% by HPLC. CAS 301836-43-1. Ref.: Rena, G., et al. 2004. EMBO Reports 5, 60. |