brd7

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 an effective and selective dual BRD7 9 PROTAC degrader (DC50s: 4.5 and 1.8 nM, respectively).

SJ46421, a PROTAC protein degrader derived from (+)-JQ-1, targets KLHDC2. It efficiently forms a stable ternary complex with KLHDC2, exhibiting an IC50 of 7.8 nM. Furthermore, SJ46421 promotes the polyubiquitination of the BD2 domain of BRD2, BRD3, or BRD4.

dBRD9 HCl is a PROTAC composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide . dBRD9 HCl is a potent and selective degrader of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). dBRD9 HCl does not degrade BRD4 or BRD7 at concentrations up to 5 μM. dBRD9 HCl displays antiproliferative effects in human AML cell lines.