| 应用 |
A cell-permeable triaryl substituted imidazolo compound that acts as a selective inhibitor of casein kinase 1 (CK1). |
| 产品介绍 |
D4476是可渗透入细胞的CK1δ抑制剂，IC90 <10 uM，最初是作为ALK5抑制剂 |
| 生化机理 |
D4476 is a cell-permeable triaryl substituted imidazolo compound that acts as a selective inhibitor of casein kinase 1 (CK1) and TGFβ RI (TGF-βtype-I receptor, ALK5). Weak inhibitor of Polycystin-1 (PKD1), p38? (p38α MAPK) and only weakly affects the activities of kinases, including Akt1 (PKB), SGK and GSK-3b. Suppresses the site-specific phosphorylation (Ser322 and Ser325) and nuclear exclusion of FKHR (FOXO1a) in H4IIE hepatoma cells. As an inhibitor of TGFβ RI, D4476 prevents Smad3 activation and suppresses TGFβ RI gene expression without cytotoxicity in A498 cells. In HeLa cells D4476 has been used to inhibit CK-1 phosphorylation of RhoB but not RhoA or RhoC activating RhoB dependent actin fiber formation. D4476 has been observed to block the Wnt-3a-induced phosphorylation and shift in electrophoretic migration of Dvl-1(dishevelled, Dvl). |
| 别名 |
D 4476;D-4476;4-[4-(2,3-二氢-1,4-苯并二氧杂环己-6-基)-5-(2-吡啶基)-1H-咪唑-2-基]苯甲酰胺;Casein Kinase I Inhibitor;D 4476;D-4476;4-(4-(2,3-Dihydrobenzo[1,4]dioxin-6-yl)-5-pyridin-2-yl-1H-imidazol-2-yl)benzamide |
