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Cat. No.: HY-172124

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PROTAC BRD4 Degrader-29

PROTAC BRD4 Degrader-29 is a potent BRD4 PROTAC degrader with a DC₅₀ of 89.4 nM. PROTAC BRD4 Degrader-29 mediates proteasomal degradation of BRD4 by bridging BRD4 and the CRBN E3 ubiquitin ligase. PROTAC BRD4 Degrader-29 can be used in cancer research.
(Pink: BRD4 ligand (HY-13030); Blue: Cereblon ligand (HY-103597); Black: linker (HY-172125)).

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

Formula: C₅₈H₆₁ClN₁₀O₉S₂
Molecular Weight:1141.75

Storage:

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

Data Sheet (276 KB)

PROTAC BRD4 Degrader-29 Chemical Structure

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Use of MCE Products

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

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

Description

PROTAC BRD4 Degrader-29 is a potent BRD4 PROTAC degrader with a DC₅₀ of 89.4 nM. PROTAC BRD4 Degrader-29 mediates proteasomal degradation of BRD4 by bridging BRD4 and the CRBN E3 ubiquitin ligase. PROTAC BRD4 Degrader-29 can be used in cancer research^[1]. (Pink: BRD4 ligand (HY-13030); Blue: Cereblon ligand (HY-103597); Black: linker (HY-172125)).

IC₅₀ & Target

^[1]

BRD4

89.4 nM (DC₅₀)

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	DC₅₀	89.4 nM	BRD4 degradation in HEK293 CRISPR HiBiT BRD4 cells assessed by Nano-Glo HiBiT assay after 18 h of incubation. BRD4 degradation in HEK293 CRISPR HiBiT BRD4 cells assessed by Nano-Glo HiBiT assay after 18 h of incubation.	39967623

In Vitro

PROTAC BRD4 Degrader-29 (Compound 7a) (0.001-10 μM; 18 h) efficiently degrades BRD4 in HEK293 CRISPR HiBiT BRD4 cells with a DC₅₀ of 89.4 nM. It also degrades the BRD4 long and BRD4 short isoforms in parental HEK293 cells, and its degradation activity can be reversed by the proteasome inhibitor MG132 (HY-13259), neddylation inhibitor MLN4924 (HY-70062), and CRBN ligand competitor Thalidomide (HY-14658)^[1].

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

Western Blot Analysis^[1]

Cell Line:

HEK293 parental cell line
Concentration:

0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
Incubation Time:

18 h
Result:

Visibly degraded both BRD4 long and BRD4 short isoforms in the range of 0.3-1 μM, and this degradation was reversed by the addition of MG132, MLN4924, or thalidomide, confirming its dependence on the proteasome and CRBN ubiquitin ligase pathways.

Chemical Information

Molecular Weight 1141.75
Formula C₅₈H₆₁ClN₁₀O₉S₂
SMILES

CC1=NN=C2N1C3=C(C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NCCNC(C5=CC=C(SCCC#CC(C6CCOCC6)N7CCC(NC(COC8=CC=CC9=C8C(N(C%10CCC(NC%10=O)=O)C9=O)=O)=O)CC7)C=C5)=O)=O)C(C)=C(C)S3
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 (276 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]. McGown A, et al. Use of Aldehyde-Alkyne-Amine Couplings to Generate Medicinal Chemistry-Relevant Linkers. ACS Med Chem Lett. 2025 Jan 25;16(2):278-284.

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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100 mg

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