brd-in-3

BRD-IN-3 is a highly potent PCAF bromodomain (BRD) inhibitor (IC50: 7 nM). It also exhibits activity against GCN5 and FALZ.

BTR2004 is a selective PROTAC degrader targeting the BET family (BRD2/3/4) proteins. It facilitates the formation of a ternary complex with BRD proteins and KLHL20, leading to ubiquitination and proteasomal degradation via the UPS pathway. BTR2004 shows potential for research in PC3 prostate cancer and MDA-MB-231 breast cancer cell lines.

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.

BRD4-Kinases-IN-3 is a dual BRD4-Kinases inhibitor that can be used as a value-added multi-targeted chemical probe for cancer therapy.

BRD PHOTAC-I-3 is a photoswitchable BET bromodomain degrader (PHOTAC, PHOtochemically TArgeting Chimera). BRD PHOTAC-I-3 comprises a ligand for an E3 ligase, a photoswitch, and the BET bromodomain targeting ligand (+)-JQ1. Exhibits cytotoxicity and degrades BRD4, BRD3 and to a lesser extent BRD2 in lymphoblast cells upon irradiation with 390 nm light, but not in the dark.