Synonyms: N-((R)-1-((1s,4S)-4-Aminocyclohexylamino)-3-(4-cyanophenyl)propan-2-yl)-2-chloro-4-methoxy-5-(5-(((R)-1-p-tolylethylamino)methyl)furan-2-yl)benzamide trihydrochloride; N-[(2R)-1-[(4-Aminocyclohexyl)amino]-3-(4-cyanophenyl)propan-2-yl]-2-chloro-4-methoxy-5-[5-({[(1R)-1-(4-methylphenyl)ethyl]amino}methyl)-2-furyl]benzamide trihydrochloride
Molecular Formula: C38H44ClN5O3 · 3HCl
Molecular Weight: 763.62
Linear Structural Formula: C38H44ClN5O3 · 3HCl
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: 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 muM). 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 muM by HTRF). To avoid potential unspecific off-target effects, concentrations above 5 muM are not recommended. BAY-460 is a companion control compound with strongly reduced ATAD2 inhibitory potency (IC50 = 16 muM by cell-based HTRF assay; no activity at 10 muM by BROMOscan).