baz2a

BAZ2-ICR is an epigenetic chemical probe and it also is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains.

GSK8573 is an inactive control compound for GSK2801, with binding activity to BRD9 (Kd of 1.04 μM).

GSK2801 is an effective, specific and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd: 136 nM) and BAZ2B(Kd: 257 nM) bromodomains.

BAZ2A/B ligand 1 (compound 1) serves as a ligand for target proteins in PROTAC applications. It can be utilized in the synthesis of dBAZ2.

dBAZ2 is a pioneering PROTAC degrader targeting BAZ2A and BAZ2B, with DC50 values of 180 nM for BAZ2A and 250 nM for BAZ2B.

dBAZ2B is a BAZ2B PROTAC degrader with a DC50 value of 19 nM. (Pink: BAZ2A/B ligand; Black: linker; Blue: CRBN Ligand)