PROTAC BRD4 Degrader-1

PROTAC BRD4 Degrader-1 is an efficacious BRD4 degrader with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression[1].

Research Areas >> Cancer

Signaling Pathways >> PROTAC >> PROTAC

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

BRD4 (BD1):41.8 nM (IC50)

PROTAC BRD4 Degrader-1 (compound 21) (2.5 μM; 24 hours) shows high inhibitory activity against the growth of human monocyte lymphoma cell line THP-1, with the IC50 value of 0.81 μM, and moderate activity against Raji and HL-60 cell lines[1]. PROTAC BRD4 Degrader-1 (1 μM; 24 hours) effectively induces the degradation of BRD4 protein and suppression of c-Myc, while pomalidomide couldn’t degrade BRD4 at the low concentration[1]. Cell Proliferation Assay[1] Cell Line: HL-60, Raji and THP-1 cell Concentration: 2.5 μM Incubation Time: 24 hours Result: Inhibited HL-60, Raji and THP-1 cell growth. Western Blot Analysis[1] Cell Line: THP-1 cell Concentration: 1 μM Incubation Time: 3 hours Result: Degraded BRD4 protein and suppressed c-Myc expression.

[1]. Zhang F, et al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.Bioorg Med Chem. 2020 Jan 1;28(1):115228.