2133360-00-4

2133360-00-4 structure

Name: PROTAC BRD4 Degrader-1
Chemical Name: PROTAC BRD4 Degrader-1
CAS Number: 2133360-00-4
Molecular Formula: C₄₀H₃₇N₉O₈
Molecular Weight: 771.78
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2020-01-23 20:05:51
Modify Date: 2024-01-11 08:36:06
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].

Name	PROTAC BRD4 Degrader-1

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> PROTAC >> PROTAC Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain
Target	BRD4 (BD1):41.8 nM (IC50)
In Vitro	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.
References	[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.