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Art. -Nr.: 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 the ubiquitination and subsequent proteasomal degradation of BRD4 by recruiting the ubiquitin E3 ligase KLHDC2. PROTAC BRD4 Degrader-3 can be used in breast cancer research.
(Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 ligand (HY-174218); Black: linker (HY-174222)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₅₄H₆₂ClN₇O₄S
Molecular Weight:940.63

Speicherung:

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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Preis

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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 the ubiquitination and subsequent proteasomal degradation of BRD4 by recruiting the ubiquitin E3 ligase KLHDC2. PROTAC BRD4 Degrader-3 can be used in breast cancer research^[1]. (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)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

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.

Related Protocols :

Breast Cancer Modeling

Chemical Information

Molecular Weight 940.63
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 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)

Verweise

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

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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