中文名称:

2018300-62-2

中文同义词:

CBP/P300苯并西泮溴结构域抑制剂(TPOP146)

英文名称:

TPOP146

英文同义词:

TPOP146;TPOP-146; TPOP 146;7-(3,5-dimethoxyphenyl)-N-[(3S)-1-methylpiperidin-3-yl]-4-propanoyl-3,5-dihydro-2H-1,4-benzoxazepine-9-carboxamide;1,4-Benzoxazepine-9-carboxamide, 7-(3,5-dimethoxyphenyl)-2,3,4,5-tetrahydro-N-[(3S)-1-methyl-3-piperidinyl]-4-(1-oxopropyl)-

CAS号:

2018300-62-2

分子式:

C27H35N3O5

分子量:

481.58

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

2018300-62-2.mol

沸点 

641.8±55.0 °C(Predicted)

密度 

1.24±0.1 g/cm3(Predicted)

酸度系数(pKa)

10.68±0.20(Predicted)

生物活性

TPOP146是选择性的CBP/P300苯并西泮溴结构域抑制剂；对CBP和BRD4的Kd值分别为134 nM和5.02 μM。

靶点

IC50: 134 nM (CBP); 5.02 μM (BRD4)

体外研究

Exposure to 1 μM TPOP146 results in a significant decrease of recovery half-life that is comparable to the construct that contained the bromodomain inactivating mutation N1168F, demonstrating that TPOP146 targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments.