BAY-850 is a chemical probe that targets ATPase family AAA domain-containing protein 2 (ATAD2) bromodomain (BD) with submicromolar affinity (Kd of 84.9 nM by MST and 120 nM by BROMOscan) and high selectivity over all other bromodomains tested (no BROMOscan hits at 10 μM). BAY-850 blocks ATAD2 BD from binding acetylated H4 peptide in cell-free assays (IC50 of 20 nM) and displaces full-length ATAD2 from chromatin in live cells (effctive conc. 1 μM by HTRF). To avoid potential unspecific off-target effects, concentrations above 5 μM are not recommended. BAY-460 is a companion control compound with strongly reduced ATAD2 inhibitory potency (IC50 = 16 μM by cell-based HTRF assay; no activity at 10 μM by BROMOscan).
Chemical probe that targets ATAD2 bromodomain (BD) with submicromolar affinity and displaces full-length ATAD2 from chromatin in live cells.
