TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with K d values of 134 nM and 5.02 μM for CBP and BRD4 .
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:IC50: 134 nM (CBP),5.02 μM (BRD4)
规格
规格或纯度
10mM in DMSO
英文名称
TPOP146
生化机理
TPOP146 是一种选择性 CBP/P300 苯并氧氮杂卓溴域抑制剂,对 CBP 和 BRD4 的 K d 值分别为 134 nM 和 5.02 μM。