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Cat. No.: HY-174210

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PROTAC BRD4 Degrader-31

PROTAC BRD4 Degrader-3 is a potent BRD4 PROTAC degrader, with DC₅₀ values of 164 nM and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-3 induces ubiquitination of BRD4 by recruiting the ubiquitin E3 ligase KLHDC2, leading to its degradation via the proteasome-dependent pathway. PROTAC BRD4 Degrader-3 can be used for research on breast cancer.

(Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 ligand (HY-174218); Black: linker (HY-174222)).

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

Formula: C₅₄H₆₂ClN₇O₄S
Molecular Weight:940.63

Storage:

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

Data Sheet (269 KB)

PROTAC BRD4 Degrader-31 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

(Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 ligand (HY-174218); Black: linker (HY-174222)).

IC₅₀ & Target

BRD4

164 nM (DC₅₀, 4 h)

BRD4

80 nM (DC₅₀, 24 h)

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

In Vitro

PROTAC BRD4 Degrader-3 (Compound 8) (0-10 μM; 4 h-24 h) degrades exogenous BRD4 in HEK293T cells^[1].
PROTAC BRD4 Degrader-3 (0.1-10 μM; 24 h) exerts a degrading effect on endogenous BRD4 in SK-BR-3 cells^[1].
PROTAC BRD4 Degrader-3 (10 μM; 24 h) exerts a proteasome-dependent BRD4 degradation effect in SK-BR-3 cells co-treated with MG-132 (HY-13259)^[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
Concentration:

0.1, 0.5, 1, 5, 10 μM
Incubation Time:

24 h
Result:

Significantly reduced the protein expression levels of endogenous BRD4 in a dose-dependent manner

Western Blot Analysis^[1]

Cell Line:

SK-BR-3
Concentration:

10 μM
Incubation Time:

24 h (co-treated with the proteasome inhibitor MG-132)
Result:

The BRD4 degradation effect caused by PROTAC BRD4 Degrader-3 was partially reversed by MG-132, indicating that the degradation is dependent on the proteasome pathway.

Chemical Information

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zhou H, et al. Targeted protein degradation by KLHDC2 ligands identified by high-throughput screening. eLife. 2025 Jun 16;14:RP106844.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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PROTAC BRD4 Degrader-31

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC BRD4 Degrader-31 Related Classifications

HY-174210 Related Classifications