PROTAC BRD4 Degrader-1

Modify Date: 2024-01-11 08:36:06

PROTAC BRD4 Degrader-1 Structure
PROTAC BRD4 Degrader-1 structure
Common Name PROTAC BRD4 Degrader-1
CAS Number 2133360-00-4 Molecular Weight 771.78
Density N/A Boiling Point N/A
Molecular Formula C40H37N9O8 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name PROTAC BRD4 Degrader-1

 PROTAC BRD4 Degrader-1 Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C40H37N9O8
Molecular Weight 771.78
Storage condition 2-8°C