VZ185

VZ185 is a chemically optimized, probe‑quality proteolysis‑targeting chimera (PROTAC) that recruits the von Hippel–Lindau (VHL) E3 ubiquitin ligase to selectively degrade the bromodomain‑containing proteins BRD9 and its close homolog BRD7, subunits of BAF/PBAF chromatin‑remodeling complexes.[2][3][11] Designed through iterative medicinal chemistry on VHL‑based degraders, VZ185 forms a ternary complex between VHL and BRD7/9, leading to ubiquitination and proteasomal degradation with single‑digit nanomolar DC50 values and rapid, profound knockdown across multiple cancer cell lines.[2][3][8][10][11] Developed as a tool compound by Boehringer Ingelheim and collaborators, it exhibits favorable in vitro and in vivo pharmacokinetic properties and is widely supplied by chemical vendors for mechanistic studies of BRD7/9 biology and epigenetic regulation rather than for clinical use.[3][8][9][11]