1. PROTAC Epigenetics
  2. PROTACs Epigenetic Reader Domain
  3. PROTAC BRD4 Degrader-31

PROTAC BRD4 Degrader-31 is a BRD4 PROTAC degrader with DC50 s of 164 and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-31 potently degrades BRD4 in cells with long acting degradation kinetics. Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 ligand (HY-174218)

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

PROTAC BRD4 Degrader-31 Chemical Structure

PROTAC BRD4 Degrader-31 Chemical Structure

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Description

PROTAC BRD4 Degrader-31 is a BRD4 PROTAC degrader with DC50 s of 164 and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-31 potently degrades BRD4 in cells with long acting degradation kinetics[1]. Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 ligand (HY-174218)

IC50 & Target[1]

BRD4

164 (4 h) nM (DC50)

BRD4

80 (80 h) nM (DC50)

In Vitro

PROTAC BRD4 Degrader-31 (Compound 8) (4-24 h) significantly degrades BRD4 with DC50, 4 h: of 164 nM and DC50, 24 h of 80 nM in HEK293T cells expressing BRD4-HiBiT transgene[1].
PROTAC BRD4 Degrader-31 (0.1-10 µM, 24 h) effectively degrades endogenous BRD4 protein through a proteasome-mediated mechanism, with maximal degradation of 94% at 24 h in SK-BR-3 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: SK-BR-3 cells
Concentration: 0.1, 0.5, 1, 5, 10 μM
Incubation Time: 24 h
Result: Degraded more than 60% of endogenous BRD4 protein at 0.1 μM.
Achieved 94% maximal degradation of endogenous BRD4 protein at 10 µM.
Partially rescued the degradation effect by MG-132 (HY-13259).
Molecular Weight

940.63

Formula

C54H62ClN7O4S

SMILES

O=C(OC)C1=C2C(C(C3CCC4C3)C4C(C5=CC(OCCC6CCN(CC7CCN(C(C[C@@H]8N=C(C9=CC=C(Cl)C=C9)C(C(C)=C(C)S%10)=C%10N%11C8=NN=C%11C)=O)CC7)CC6)=CC=C5)N2)=CC=C1

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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Product Name:
PROTAC BRD4 Degrader-31
Cat. No.:
HY-174210
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