brd7 in 1

BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), interacts with a VHL ligand via a linker to form the PROTAC VZ185 (targeting BRD7/9 with DC50 values of 4.5 and 1.8 nM, respectively)[1].

BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), forms PROTAC VZ185 via linkage to a VHL ligand, demonstrating potent activity against BRD7/9 with DC50 values of 4.5 and 1.8 nM, respectively [1].

VZ185 is a potent, fast-acting, and selective von Hippel–Lindau–based dual degrader probe targeting BRD9 and BRD7 with DC50 values of 4.5 nM and 1.8 nM, respectively. VZ185 displays marked cytotoxicity in EOL-1 and A-402 cell lines with EC50 values of 3 nM and 40 nM, enabling advanced studies of chromatin remodeling, targeted protein degradation, and cancer cell dependency on SWI/SNF complex components.