VZ 185

VZ 185 is a proteolysis-targeting chimera (PROTAC) composed of a von Hippel-Lindau (VHL) ligand and bromodomain-containing protein 7 (BRD7)- and BRD9-binding ligand. It is selective for BRD7 and BRD9 over 6,273 other proteins at 100 nM. VZ 185 degrades BRD7 and BRD9 with half-maximal degradation concentration (DC50) values of 4. and 1. nM, respectively, in a cell-free assay. It decreases BRD7 and BRD9 levels in HeLa cells by 10 and 14%, respectively, when used at a concentration of 1 µM. VZ 185 reduces the proliferation of EoL-1 leukemia and A-204 sarcoma cells (IC50s = 3. and 39 nM, respectively).. Solulibility: DMSO: Slightly soluble: 0.1-1 mg/ml: .