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
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
BRD4 |
In Vitro
PROTAC BRD4 Degrader-33 (compound Y1106) at 5 μM degrades BRD4 and downregulates the expression of PD-L1 protein in 4T1 tumor cells[1].
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.
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Cell Line:4T1 mouse breast cancer cells, HEK-293T human embryonic kidney cells
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Concentration:0.01, 0.1, 1, 5, 10 μM
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Incubation Time:12 h
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (female, subcutaneous implantation of 4T1 cells, tumors grown to ~50 mm3)[1]
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Dosage:5 mg/kg
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Administration:i.v.; once daily
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Result:Showed less effective tumor inhibition and immune remodeling compared to combined Y952 + J558 fragments.
Exhibited no significant body weight loss.
Chemical Information
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Molecular Weight 1106.64
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Formula C51H48ClN11O10S3
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC BRD4 Degrader-33 Related Classifications
HY-174811 Related Classifications
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