PROTAC BRD4 Degrader-47
PROTAC BRD4 Degrader-47 is a heterobifunctional PROTAC that selectively degrades BRD4 in a SYVN1-dependent manner, with a DC50 of 0.93 μM. PROTAC BRD4 Degrader-47 can be used in cancer-related research such as breast cancer.
(Pink: BRD4 ligand (HY-78695); Blue: Ligands for E3 Ligase ligand (HY-B1415); Black: linker (HY-184457)).
For research use only. We do not sell to patients.
- Formula: C42H42Cl2N6O3S
- Molecular Weight:781.79
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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
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- References
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Biological Activity
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BRD4 0.93 μM (DC50) |
PROTAC BRD4 Degrader-47 (compound 27) (20 h) dose-dependently degrades HiBit-BRD4 in CRISPR/Cas9-engineered HEK293T cells with a DC50 of 0.93 μM[1].
PROTAC BRD4 Degrader-47 (0-10.0 μM; 20 h) dose-dependently degrades endogenous BRD4 in native HEK293T cells with a DC50 of 0.28 μM and 90.7% maximal degradation[1].
PROTAC BRD4 Degrader-47 induces ternary complex formation between Flag-tagged BRD4 and SYVN1 in HEK293T cells[1].
PROTAC BRD4 Degrader-47 (1 μM; 2 h)-induced BRD4 degradation in HEK293T cells is dependent on SYVN1 expression, as degradation is lost in SYVN1-knockdown cells and restored by SYVN1 re-expression[1].
PROTAC BRD4 Degrader-47 (1 μM; 20 h) selectively degrades BRD4 over BRD2 and BRD3 in HEK293T cells, as shown by TMT-based quantitative proteomics[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:native HEK293T cells
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Concentration:0, 0.01, 0.05, 0.1, 1, 5, 10.0 μM
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Incubation Time:20 h
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Result:Induced significant degradation of endogenous BRD4 in a dose-dependent manner, with a DC50 of 0.28 μM and a maximal degradation efficacy (Dmax) of 90.7%.
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Cell Line:HEK293T cells
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Concentration:1 μM, 1 μM with 5 μM MG132
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Incubation Time:2 h
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Result:Induced BRD4 degradation 2 hours after treatment.
Was blocked from inducing BRD4 degradation upon co-treatment with MG132, confirming dependence on proteasome activity.
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Cell Line:HEK293T cells
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Concentration:1 μM, 1 μM with 5 μM JQ1, 1 μM with 5 μM clofibramide 8
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Incubation Time:2 h
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Result:Induced BRD4 degradation when treated alone.
Was blocked from inducing BRD4 degradation upon addition of JQ1 or clofibramide 8, confirming requirement for engagement of both BRD4 and SYVN1.
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Cell Line:shRNA-transduced HEK293T cells (control shRNA, SYVN1-targeting shRNA, SYVN1-targeting shRNA with shRNA-resistant V5-tagged SYVN1)
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Concentration:1 μM
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Incubation Time:2 h
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Result:Failed to induce BRD4 degradation in SYVN1-knockdown cells, while induced efficient degradation in shCTRL cells.
Restored ability to induce BRD4 degradation in SYVN1-knockdown cells upon re-expression of V5-tagged SYVN1.
Chemical Information
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Molecular Weight 781.79
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Formula C42H42Cl2N6O3S
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SMILES
CC(C)(OC1=CC=C(Cl)C=C1)C(NCC2=CC=C(C#CCCCCNC(C[C@H]3C4=NN=C(C)N4C5=C(C(C)=C(C)S5)C(C6=CC=C(Cl)C=C6)=N3)=O)C=C2)=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-47 Related Classifications
HY-184455 Related Classifications
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