dBRD4-BD1

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].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

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]. Western Blot Analysis[1] Cell Line: MM.1S cells Concentration: 25, 5, 1, 0.2, 0.04, 0.008, 0.0016 nM and 320 pM, 64 pM Incubation Time: 24 hours Result: Degraded BDR4 in a dose-dependent manner. Western Blot Analysis[1] Cell Line: MM.1S cells Concentration: 5 μM Incubation Time: 0, 0.5, 1, 2, 4, 8, 12, 24, 30, 36, 48, 72 hours Result: Increased the protein amount of BRD2 and BRD3 without decreasing cMyc protein level in 4 hr period.

[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.