中文名 | D4476 |
英文名 | D4476 |
别名 | D4467游离 化合物D 4476 CK1抑制剂(D4476) 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 4-(4-(2,3-二氢苯并[B][1,4]二氧杂环己烷基-6-基)-5-(吡啶-2-基)-1H-咪唑-2-基)苯甲酰胺 |
英文别名 | D4476 D-4476 D 4476 4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE 4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide Benzamide,4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]- 4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide D4476 |
CAS | 301836-43-1 |
化学式 | C23H18N4O3 |
分子量 | 398.41 |
密度 | 1.338±0.06 g/cm3(Predicted) |
沸点 | 675.0±55.0 °C(Predicted) |
溶解度 | DMSO: ~ 20毫克/毫升 |
酸度系数 | 10.16±0.10(Predicted) |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | light yellow |
体外研究 | D4476 is a potent and rather selective inhibitor of CK1 in vitro and in cells. In H4IIE hepatoma cells, D4476 specifically inhibits the phosphorylation of endogenous forkhead box transcription factor O1a (FOXO1a) on Ser322 and Ser325 within its MPD, without affecting the phosphorylation of other sites. CK1δ assayed at 0.1 mM ATP using a phosphorylated peptide TFRPRTSpSNASTIS corresponding to residues 312–325 of FOXO1a is inhibited with an IC 50 value of 0.3 μM. The IC 50 value for CK1δ decreases progressively as the concentration of ATP is lowered, indicating that D4476 is an ATP-competitive inhibitor of CK1. CK1. |
WGK Germany | 3 |
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