| Identification | Back Directory | [Name]
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 | [Synonyms]
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]- | [Molecular Formula]
C50H53F3N8O9 | [MOL File]
2839318-19-1.mol | [Molecular Weight]
967 |
| Hazard Information | Back Directory | [Description]
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. | [Uses]
dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1[1]. | [References]
[1] Divakaran A, et al. Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader. ACS Med Chem Lett. 2022 Sep 29;13(10):1621-1627. DOI:10.1021/acsmedchemlett.2c00300 |
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