p300 bromodomain-in-1

P300 bromodomain-IN-1 is a potent inhibitor of p300 (EP300) bromodomain (IC50: 49 nM). p300 bromodomain-IN-1 blocks c-Myc expression and induces cell cycle arrest at G1 G0 phase and apoptosis in OPM-2 cells. apoptosis).

Inobrodib (CBP-IN-1) is a potent inhibitor of p300 CBP bromodomain.

I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. I-CBP112 targets the CBP p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating poten

JET-209 is a potent proteolysis-targeting chimera (PROTAC) that effectively degrades CBP p300, exhibiting half-maximal degradation concentration (DC50) values of 0.05 nM for CBP and 0.2 nM for p300. The compound comprises lenalidomide (the cereblon ligand), a connecting linker, and GNE-207 (the bromodomain inhibitor). JET-209 is utilized in cancer research [1].