产品描述:
D 4476 is a cell-permeant inhibitor of casein kinase 1 (CK1; IC50 = 200 nM from S. pombe,{17330} 300 nM for CK1δ{17331}). It is a less effective inhibitor of PKD1 (IC50 = 9.1 μM) and p38α MAPK (IC50 = 5.8 μM), and only weakly affects the activities of a panel of kinases tested.{17331} D 4476 blocks CK1-mediated phosphorylation of FOXO1a,{17330} RhoB,{17333} and p53.{17334} As an inhibitor of ALK5, D 4476 prevents Smad3 activation and suppresses TGF-β1-induced gene expression without cytotoxicity in A498 cells.{16928}