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

中文同义词:

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;CK1抑制剂(D4476)

英文名称:

4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE

英文同义词:

4-(4-(2,3-DIHYDROBENZO[1,4]DIOXIN-6-YL)-5-PYRIDIN-2-YL-1H-IMIDAZOL-2-YL)BENZAMIDE;D4476;4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide;Casein Kinase I Inhibitor;4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide D4476;Casein Kinase I Inhibitor, D4476;D4476;D 4476;D-4476;Benzamide,4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]-

CAS号:

301836-43-1

分子式:

C23H18N4O3

分子量:

398.41

EINECS号:

相关类别:

细胞生物学试剂;小分子抑制剂;小分子抑制剂，天然产物;Inhibitors;Signalling

Mol文件:

301836-43-1.mol

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 

DMSO: ~20mg/mL

形态

solid

酸度系数(pKa)

10.16±0.10(Predicted)

颜色

light yellow

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 )

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.

WGK Germany 

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