cis-VZ185 is a VHL-based PROTACs degrader with the activity of degrading BRD9 and BRD7. cis-VZ185 can be optimized from suboptimal compounds by optimizing the connection mode and linker, and has efficient, rapid and selective degradation of BRD9 and its homologous protein BRD7.
cisVZ185 is the inactive cis-isomer of and the recommended negative control for the potent and selective dual BRD7 and BRD9 degrader VZ185.
[1] Iterative design and optimization of initially inactive proteolysis targeting chimeras (PROTACs) identify VZ185 as a potent, fast, and selective von Hippel–Lindau (VHL)…