2839318-19-1
中文名称
化合物 DBRD4-BD1
英文名称
Acetamide, 2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-N-[2-[2-[2-[4-[5-[2-[2-methyl-5-(1-methylethyl)phenoxy]-4-pyrimidinyl]-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]-1-piperidinyl]ethoxy]ethoxy]ethyl]-
CAS
2839318-19-1
分子式
C50H53F3N8O9
分子量
967
MOL 文件
2839318-19-1.mol
2839318-19-1 结构式
基本信息
中文别名
化合物 DBRD4-BD1 英文别名
Acetamide, 2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-N-[2-[2-[2-[4-[5-[2-[2-methyl-5-(1-methylethyl)phenoxy]-4-pyrimidinyl]-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]-1-piperidinyl]ethoxy]ethoxy]ethyl]-应用领域
用途一
dBRD4-BD1 is a selective BRD4 bromodomain inhibitor. dBRD4-BD1 can selectively degrade BRD4 (DC50 = 280 nM). Notably, dBRD4-BD1 upregulates BRD2/3, a result not observed with degraders using pan-BET ligands. Designing BRD4 selectivity up front enables analysis of BRD4 biology without wider BET-inhibition and simplifies designing BRD4-selective heterobifunctional molecules, such as degraders with new E3 recruiting ligands or for additional probes beyond degraders.