BAY-850是三磷酸腺苷酶家族蛋白2(ATAD2)的选择性有效抑制剂，其IC50值为166nM。
BAY-850 is a potent and isoform selective ATPase family AAA domain-containing protein 2 (ATAD2) inhibitor, with an IC50 of 166 nM.
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[1].
[1]. Fernández-Montalván AE, et al. Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action. ACS Chem Biol. 2017 Nov 17;12(11):2730-2736.
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