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Cat. No.: HY-174811

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PROTAC BRD4 Degrader-33

PROTAC BRD4 Degrader-33 is a BRD4 PROTAC degrader that recruits CRBN. PROTAC BRD4 Degrader-33 downregulates PD-L1 expression, inhibits tumor cell proliferation and tumor growth in mice by inducing ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-33 can be used in the research of breast cancer.
(Pink: BRD4 ligand (HY-174812); Blue: Cereblon ligand (HY-10984); Black: linker).

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

Formula: C₅₁H₄₈ClN₁₁O₁₀S₃
Molecular Weight:1106.64

Storage:

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

Data Sheet (276 KB)

PROTAC BRD4 Degrader-33 Chemical Structure

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Use of MCE Products

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

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

Description

PROTAC BRD4 Degrader-33 is a BRD4 PROTAC degrader that recruits CRBN. PROTAC BRD4 Degrader-33 downregulates PD-L1 expression, inhibits tumor cell proliferation and tumor growth in mice by inducing ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-33 can be used in the research of breast cancer^[1]. (Pink: BRD4 ligand (HY-174812); Blue: Cereblon ligand (HY-10984); Black: linker).

IC₅₀ & Target

^[1]

BRD4

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

In Vitro

Immune Tolerance & ImmunosuppressionAnti-cancerOthers

Immune Tolerance & Immunosuppression

Anti-cancer

PROTAC BRD4 Degrader-33 (compound Y1106) at 5 μM degrades BRD4 and downregulates the expression of PD-L1 protein in 4T1 tumor cells^[1].

Others

PROTAC BRD4 Degrader-33 (0.01-10 μM; 12 h) induces concentration-dependent degradation of BRD4 protein in 4T1 tumor cells and normal HEK-293T cells, with significant degradation effects observed at a concentration of 5 μM^[1].
PROTAC BRD4 Degrader-33 (5 μM; 24 h) reduces BRD4 protein levels in 4T1 multicellular tumor spheroids (MCTSs), but its limited permeability results in poor degradation efficacy in the central region of the spheroids^[1].

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

Western Blot Analysis^[1]

Cell Line:

4T1 mouse breast cancer cells, HEK-293T human embryonic kidney cells
Concentration:

0.01, 0.1, 1, 5, 10 μM
Incubation Time:

12 h
Result:

Caused a concentration-dependent decrease in BRD4 protein levels in both 4T1 tumor cells and HEK-293T normal cells.
Confirmed significant BRD4 reduction in both cell lines at the 5 μM concentration.

In Vivo

Anti-cancerAdaptive Immunity

Anti-cancer

Adaptive Immunity

PROTAC BRD4 Degrader-33 (Y1106) (5 mg/kg; intravenous injection; once daily) exhibits weaker tumor suppression and immune microenvironment remodeling activity than the combined administration of Y952 + J558 fragments in BALB/c mice subcutaneously inoculated with 4T1 breast cancer cells^[1].

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

Animal Model:

BALB/c mice (female, subcutaneous implantation of 4T1 cells, tumors grown to ~50 mm³)^[1]
Dosage:

5 mg/kg
Administration:

i.v.; once daily
Result:

Showed less effective tumor inhibition and immune remodeling compared to combined Y952 + J558 fragments.
Exhibited no significant body weight loss.

Related Protocols :

Chemical Information

Molecular Weight 1106.64
Formula C₅₁H₄₈ClN₁₁O₁₀S₃
SMILES

O=C(CCC1N(C2=O)C(C3=C2C(NC(COCCOCCOCCNC(C4N=C(C5=NC6=CC=C(NC(C[C@@H]7C8=NN=C(N8C(S9)=C(C(C)=C9C)C(C(C=C%10)=CC=C%10Cl)=N7)C)=O)C=C6S5)SC4)=O)=O)=CC=C3)=O)NC1=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 (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]. Sun C, et al. Enzyme-Activated Orthogonal Proteolysis Chimeras for Tumor Microenvironment-Responsive Immunomodulation. Angewandte Chemie (International ed. in English). 2025 May 26;64(22):e202423057. [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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