cbp/p300-in-3

CBP/p300-IN-3 (P300/CBP-IN-3) is an inhibitor of p300/CBP histone acetyltransferase.

CZL-077 is a potent, highly selective, and orally active p300/CBP bromodomain (BRD) inhibitor, with p300 IC50 at 0.034 μM and CBP IC50 at 0.052 μM, demonstrating strong selectivity for the BRD of BET proteins (BRD2/3/4). This compound effectively inhibits the growth of OPM-2 and 22RV1 cells, with IC50 values of 0.024 μM and 5.6 μM, respectively. In xenograft mouse models of OPM-2 and 22RV1, CZL-077 exhibits anti-tumor activity. CZL-077 is applicable for research in multiple myeloma and prostate cancer.

CBP/p300 ligand-Linker Conjugate 3 is a target protein ligand-linker conjugate, comprising a CBP/p300 ligand and a PROTAC linker, capable of recruiting E3 ligase. This compound is utilized in synthesizing PROTACCBP/P300 Degrader-2.

CBP/p300 ligand 10 (Compound 3-E) functions as a CBP/P300 degrader. It also serves as a ligand for Target Protein for PROTACs, and is utilized in the synthesis of PROTACCBP/P300 Degrader-2.

CBP/p300-IN-15 (compound 13a) is a potent inhibitor of p300 (IC50: 2.5 nM) and CBP (IC50: 28.0 nM). It inhibits OVCAR-3 cells (EC50: 0.865 μM) and A2780 cells (EC50: 2.71 μM). CBP/p300-IN-15 can be used to study ovarian cancer.