BY27

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].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

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)

[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.