2018300-62-2
2018300-62-2 结构式
基本信息
中文别名
CBP/P300苯并西泮溴结构域抑制剂(TPOP146) 英文别名
TPOP146TPOP-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)-
物理化学性质
沸点641.8±55.0 °C(Predicted)
密度1.24±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO : ≥ 100 mg/mL (207.65 mM)
酸度系数(pKa)10.68±0.20(Predicted)
形态Solid
颜色White to off-white
常见问题列表
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.