301836-43-1
中文名称
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
英文名称
4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE
CAS
301836-43-1
分子式
C23H18N4O3
分子量
398.41
MOL 文件
301836-43-1.mol
更新日期
2023/09/24 21:48:30
301836-43-1 结构式
基本信息
中文别名
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
英文别名
D4476D4467
CS-1031
D4476 (D-4476)
D4476
D 4476
D-4476
Casein Kinase I Inhibitor
Casein Kinase I Inhibitor, D4476
CASEIN KINASE I INHIBITOR
D 4476
D-4476
Casein Kinase I Inhibitor, D4476 - CAS 301836-43-1 - Calbiochem
4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE
所属类别
生物化工：激动剂抑制剂物理化学性质
沸点675.0±55.0 °C(Predicted)
密度1.338±0.06 g/cm3(Predicted)
储存条件2-8°C
溶解度二甲基亚砜：20 毫克/毫升
酸度系数(pKa)10.16±0.10(Predicted)
形态固体
颜色淡黄色
常见问题列表
生物活性
D4476是具有有效性，选择性和细胞渗透性的CK1抑制剂，其在体外实验的IC50值为0.3 μM。靶点
|
CK1 0.3 μM (IC 50 ) |
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.