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Cat. No.: HY-175225

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PROTAC BRD4 Degrader-37

PROTAC BRD4 Degrader-37 is a BRD4 PROTAC degrader with a DC₅₀ of 36.4 nM. PROTAC BRD4 Degrader-37 recruits the E3 ubiquitin ligase TRIM21, binds to the PRYSPRY domain of TRIM21 (K_D = 123 nM), and thereby mediates the ubiquitination and degradation of BRD4. PROTAC BRD4 Degrader-37 exhibits cytotoxicity against PANC-1 cells (GI₅₀ = 0.282 μM). PROTAC BRD4 Degrader-37 can be used in studies related to pancreatic cancer.
(Pink: BRD4 ligand (HY-175242); Blue: TRIM21 E3 ligase ligand; Black: linker).

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

Formula: C₄₆H₅₅N₃O₆S₂
Molecular Weight:810.08

Storage:

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

Data Sheet (271 KB)

PROTAC BRD4 Degrader-37 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
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Classifications
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Biological Activity

Description

PROTAC BRD4 Degrader-37 is a BRD4 PROTAC degrader with a DC₅₀ of 36.4 nM. PROTAC BRD4 Degrader-37 recruits the E3 ubiquitin ligase TRIM21, binds to the PRYSPRY domain of TRIM21 (K_D = 123 nM), and thereby mediates the ubiquitination and degradation of BRD4. PROTAC BRD4 Degrader-37 exhibits cytotoxicity against PANC-1 cells (GI₅₀ = 0.282 μM). PROTAC BRD4 Degrader-37 can be used in studies related to pancreatic cancer^[1]. (Pink: BRD4 ligand (HY-175242); Blue: TRIM21 E3 ligase ligand; Black: linker).

IC₅₀ & Target^[1]

BRD4

36.4 nM (DC₅₀)

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
PANC-1	DC₅₀	36.4 nM	BRD4 degradation in human PANC-1 cells measured via High-Content Analysis (HCA) assay after 24-hour treatment. BRD4 degradation in human PANC-1 cells measured via High-Content Analysis (HCA) assay after 24-hour treatment.	40623734
PANC-1	GI₅₀	0.282 μM	Antiproliferative activity against human PANC-1 cells assessed in an antiproliferation assay. Antiproliferative activity against human PANC-1 cells assessed in an antiproliferation assay.	40623734
PANC-1	DC₅₀	2.847 nM	BRD4 protein degradation in human PANC-1 cells assessed via High Content Analysis (HCA) assay following 24 h incubation. BRD4 protein degradation in human PANC-1 cells assessed via High Content Analysis (HCA) assay following 24 h incubation.	40623734

In Vitro

PROTAC BRD4 Degrader-37 (TrimTAC-2) (0.01-1000000 nM; 24 h) dose-dependently degrades BRD4 in PANC-1 cells with a DC₅₀ of 36.4 nM and a Dmax of 73% after 24-hour treatment, as measured by HCA assay^[1].
PROTAC BRD4 Degrader-37 (TrimTAC-2) (0.001-100 μM) forms a dose-dependent ternary complex with 100 nM BRD4 and 100 nM His-TRIM21 in a cell-free FRET assay^[1].
PROTAC BRD4 Degrader-37 (0.01-100000 nM; 24 h) (TrimTAC-2 / HGC-673) potently degrades BRD4 in PANC-1 cells with a DC₅₀ of 2.847 nM and a maximum degradation of 73% after 24-hour treatment.

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

Chemical Information

Molecular Weight 810.08
Formula C₄₆H₅₅N₃O₆S₂
SMILES

CSC1=CC=CC=C1C2=CC(S(C)(=O)=O)=C(C=C2)C(N(CC3CCCCC3)CCCCCCCNC(C4=CC5=C(C(C)=CC(C6=CN(C(C(C)=C6)=O)C)=C5)O4)=O)=O
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 (271 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]. Zhang L, et al. TRIM21-Driven Degradation of BRD4: Development of Heterobifunctional Degraders and Investigation of Recruitment and Selectivity Mechanisms. Journal of chemical information and modeling. 2025 Jul 28;65(14):7584-7604. [Content Brief]

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

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PROTAC BRD4 Degrader-37

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms