1. PROTAC
    Epigenetics
  2. PROTAC
    Epigenetic Reader Domain
  3. PROTAC BRD4 Degrader-1

PROTAC BRD4 Degrader-1 

Cat. No.: HY-133131
Handling Instructions

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.

For research use only. We do not sell to patients.

PROTAC BRD4 Degrader-1 Chemical Structure

PROTAC BRD4 Degrader-1 Chemical Structure

CAS No. : 2133360-00-4

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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].

IC50 & 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.
Molecular Weight

771.78

Formula

C₄₀H₃₇N₉O₈

CAS No.

2133360-00-4

SMILES

O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)COCCN4N=NC(CN5C(N(C)C6=C(C=C(C7=C(C)ON=C7C)C=C6)C5C8=CC=CC=C8)=O)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PROTAC BRD4 Degrader-1PROTACEpigenetic Reader DomainProteolysis-targeting chimeraHL-60 Raji THP-1cellInhibitorinhibitorinhibit

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PROTAC BRD4 Degrader-1
Cat. No.:
HY-133131
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