Description
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 VitroExposure 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.Form:SolidIC50& Target:IC50: 134 nM (CBP),5.02 µM (BRD4)