301836-43-1
中文名稱
4-[4-(2,3-二氫-1,4-苯并二氧雜環(huán)己-6-基)-5-(2-吡啶基)-1H-咪唑-2-基]苯甲酰胺
英文名稱
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
2024/06/17 17:25:41
301836-43-1 結(jié)構(gòu)式
基本信息
中文別名
CK1抑制劑(D4476)4-[4-(2,3-二氫-1,4-苯并二氧雜環(huán)己-6-基)-5-(2-吡啶基)-1H-咪唑-2-基]苯甲酰胺
英文別名
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
所屬類別
生物化工：激動劑抑制劑物理化學性質(zhì)
沸點675.0±55.0 °C(Predicted)
密度1.338±0.06 g/cm3(Predicted)
儲存條件2-8°C
溶解度二甲基亞砜：20 毫克/毫升
酸度系數(shù)(pKa)10.16±0.10(Predicted)
形態(tài)固體
顏色淡黃色
常見問題列表
生物活性
D4476是具有有效性，選擇性和細胞滲透性的CK1抑制劑，其在體外實驗的IC50值為0.3 μM。靶點
|
CK1 0.3 μM (IC 50 ) |
體外研究
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.