PROTAC BRD4 Degrader-40
PROTAC BRD4 Degrader-40 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-40 binds to Cereblon and recruits the CRL4CRBN E3 ubiquitin ligase complex, mediates BRD4 degradation via the ubiquitin-proteasome pathway, and does not induce the degradation of classic CRBN neo-substrates IKZF1 and IKZF3. PROTAC BRD4 Degrader-40 induces BRD4 degradation in cancer cells. PROTAC BRD4 Degrader-40 can be used in research related to diffuse large B-cell lymphoma and acute myeloid leukemia.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-163927); Black: linker).
For research use only. We do not sell to patients.
- Formula: C39H34ClN9O4S
- Molecular Weight:760.26
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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
Biological Activity
Description
IC50 & Target
[1]|
BRD4 |
Cereblon |
In Vitro
PROTAC BRD4 Degrader-40 (Compound 5Y-3) (1-10000 nM; 1-24 h) potently depletes BRD4 in SU-DHL-4 cells via the ubiquitin-proteasome pathway[1].
PROTAC BRD4 Degrader-40 (1-1000 nM; 24 h) potently depletes BRD4 in MV-4-11 cells[1].
PROTAC BRD4 Degrader-40 (100 nM; 8 h) does not induce degradation of CRBN neo-substrates IKZF1 or IKZF3 in SU-DHL-4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human diffuse large B-cell lymphoma SU-DHL-4 cells
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Concentration:1, 10, 100, 1000 and 10000 nM (24 h incubation); 100 nM (1-12 h incubation); 100 nM (24 h incubation, with 1 h pre-incubation of 1 μM proteasome inhibitor Bortezomib (HY-10227), proteasome inhibitor MG1329 (HY-13259), or neddylation inhibitor MLN4924 (HY-70062))
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Incubation Time:24 h (1-10000 nM); 1 h, 3 h, 6 h, 9 h, 12 h (100 nM); 24 h (100 nM with 1 h pre-incubation of inhibitors)
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Result:Completely depleted BRD4 protein after 24 h treatment with 100 nM.
Initiated BRD4 degradation after 6 h of 100 nM treatment, with most BRD4 depleted by 12 h.
Rescued BRD4 from degradation when co-treated with proteasome inhibitors Bortezomib or MG132 (HY-13259), or neddylation inhibitor MLN4924 (HY-70062).
Required 100 nM or higher concentrations for effective degradation after 24 h in SU-DHL-4 cells.
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Cell Line:human acute myeloid leukemia MV-4-11 cells
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Concentration:1, 3, 10, 30, 100, 300 and 1000 nM
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Incubation Time:24 h
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Result:Effectively depleted BRD4 protein at concentrations as low as 10 nM after 24 h treatment.
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Cell Line:human diffuse large B-cell lymphoma SU-DHL-4 cells
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Concentration:100 nM
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Incubation Time:8 h
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Result:Did not induce degradation of the CRBN neosubstrates IKZF1 or IKZF3 after treatment.
Chemical Information
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Molecular Weight 760.26
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Formula C39H34ClN9O4S
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SMILES
O=C(N/N=C\C1=CC=C(C2=C(N3C)C(N(C(CC4)C(NC4=O)=O)C3=O)=CC=C2)C=C1)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5
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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-40 Related Classifications
HY-177730 Related Classifications
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