BAY-850

Research use only, not for human use.

BAY-850 (BAY 850, BAY850) is a potent, isoform selective, cellularly active ATAD2 bromodomain inhibitor with binding IC50 of 166 nM in TR-FRET assay.

BAY-850 (BAY 850, BAY850) is a potent, isoform selective, cellularly active ATAD2 bromodomain inhibitor with binding IC50 of 166 nM in TR-FRET assay; shows no inhibitory activity in a panel of 354 kinases and only modest effects on a few GPCRs; displaces a tetra-acetylated H4 peptide with an IC50 of 22 nM, and the tetra-acetylated peptides with IC50 of 115 nM; pecifically induces ATAD2 bromodomain dimerization and prevents interactions with acetylated histones in vitro, as well as with chromatin in cells.

BAY-850 competes with the binding of a mono-acetylated Histone H4 N-terminal peptide to ATAD2 BD with an IC50 of 166 nM measured in TR-FRET assay. BAY-850 displaces the tetra-acetylated peptide with an IC50 of 157 nM and a KD of 115 nM respectively. The unprecedented isoform selectivity of BAY-850 suggests a different mode of action to those exhibited by canonical BD inhibitors.

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BAY 850 | BAY850

Chromatin/Epigenetic

Bromodomain

Bromodomain

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2099142-76-2

654.252

C38H44ClN5O3

>98% (HPLC)

10 mM in DMSO

O=C(N[C@H](CC1=CC=C(C#N)C=C1)CNC2CCC(N)CC2)C3=CC(C4=CC=C(CN[C@@H](C5=CC=C(C)C=C5)C)O4)=C(OC)C=C3Cl

N-((R)-1-(((1s,4S)-4-aminocyclohexyl)amino)-3-(4-cyanophenyl)propan-2-yl)-2-chloro-4-methoxy-5-(5-((((R)-1-(p-tolyl)ethyl)amino)methyl)furan-2-yl)benzamide

(-20℃)

With Ice Pack

≥ 2 years