| 货号 | 13305-1mg |
| 描述 | D 4476 is a cell-permeant inhibitor of casein kinase 1 (CK1; IC50 = 200 nM from S. pombe,1 300 nM for CK1δ2). 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.2 D 4476 blocks CK1-mediated phosphorylation of FOXO1a,1RhoB,3 and p53.4 As an inhibitor of ALK5, D 4476 prevents Smad3 activation and suppresses TGF-β1-induced gene expression without cytotoxicity in A498 cells.5 |
| 别名 | Casein Kinase I Inhibitor; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Rena, G.,Bain, J.,Elliot, M., et al. D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO reports 5(1), 60-65 (2004). 2.Bain, J.,Plater, L.,Elliot, M., et al. The selectivity of protein kinase inhibitors: A further update. Biochemistry Journal 408, 297-315 (2007). 3.Tillement, V.,Lajoie-Mazenc, I.,Casanova, A., et al. Phosphorylation of RhoB by CK1 impedes actin stress fiber organization and epidermal growth factor receptor stabilization. Experimental Cell Research 314, 2811-2821 (2008). 4.MacLaine, N.J.,Oster, B.,Bundgaard, B., et al. A central role for CK1 in catalyzing phosphorylation of the p53 transactivation domain at serine 20 after HHV-6B viral infection. The Journal of Biological Chemisty 283(42), 28563-28573 (2008). 5.Callahan, J.F.,Burgess, J.L.,Fornwald, J.A., et al. Identification of novel inhibitors of the transforming growth factor ß1 (TGF-ß1) type 1 receptor (ALK5). Journal of Medicinal Chemistry 45(5), 999-1001 (2002). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 398.4 |
| 分子式 | C23H18N4O3 |
| CAS号 | 301836-43-1 |
| 稳定性 | ≥ 2 years |
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