| Identification | Back Directory | [Name]
BY27 | [CAS]
2247236-59-3 | [Synonyms]
BY27
4H-[1,2,4]Triazolo[4,3-a][1]benzazepin-6-amine, N-(4-chlorophenyl)-5,6-dihydro-1-methyl-8-(1-methyl-1H-pyrazol-4-yl)-, (6R)- | [Molecular Formula]
C22H21ClN6 | [MDL Number]
MFCD32201100 | [MOL File]
2247236-59-3.mol | [Molecular Weight]
404.9 |
| Hazard Information | Back Directory | [Description]
BY27 is a novel potent and selective BET BD2 inhibitor. | [Uses]
BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity[1]. | [IC 50]
BRD2 BD2: 3.1 nM (Ki); BRD2 BD1: 95.5 nM (Ki); BRD3 BD2: 5.3 nM (Ki); BRD3 BD1: 77.9 nM (Ki); BRD4 BD2: 7.3 nM (Ki); BRD4 BD1: 80 nM (Ki); BRD2 BD2: 1.2 nM (Kd); BRD2 BD1: 45 nM (Kd); BRD3 BD2: 2.6 nM (Kd); BRD3 BD1: 12 nM (Kd); BRD4 BD2: 3.5 nM (Kd); BRD4 BD1: 26 nM (Kd); BRDT BD2: 3 nM (Kd); BRDT BD1: 64 nM (Kd) | [References]
[1] Chen D, et al. Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins. Eur J Med Chem. 2019 Aug 21;182:111633. DOI:10.1016/j.ejmech.2019.111633 |
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