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.
dBRD4-BD1 (64 pM-25 nM; 24 h) degrades BDR4 in a dose-dependent manner[1].dBRD4-BD1 (5 μM; 0-72 h) increases the protein level of BRD2 and BRD3[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.
















