PROTAC BET Degrader-14
PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC50 = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC50 = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma.
(Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-149452); Black: linker (HY-179587)).
For research use only. We do not sell to patients.
- Formula: C59H73ClN12O9S
- Molecular Weight:1161.80
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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
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BRD4 130 nM (DC50) |
BRD4 40 nM (DC50) |
BRD2 |
BRD3 |
PROTAC BET Degrader-14 (Compound 105B) (0.01-10 μM, 24 h) dose-dependently degrades BRD4 in U2OS osteosarcoma cells[1].
PROTAC BET Degrader-14 (10 nM, 0-24 h) induces rapid degradation in U2OS osteosarcoma cells, although the effect may rebound due to BRD4 resynthesis[1].
PROTAC BET Degrader-14 (0.01 nM-1 μM, 24 h) reduces c-Myc and RUNX2 levels in U2OS osteosarcoma cells[1].
PROTAC BET Degrader-14 (0.51 nM-10) reduces KRT14 levels in KYSE180 esophageal squamous cell carcinoma cells but does not degrade BRDT[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U2OS osteosarcoma cells
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Concentration:10 nM
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Incubation Time:0 h, 0.5 h, 1 h, 1.5 h, 2 h, 4 h, 6 h, 8 h, 24 h
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Result:BRD4 degradation occurs within 4 hours and rebounds after 24 hours.
Chemical Information
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Molecular Weight 1161.80
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Formula C59H73ClN12O9S
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SMILES
O=C(C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C(C(C)=C(C)S3)=C3N4C1=NN=C4C)NCCOCCOCCOCCOCCOCCOCCOCCOCC5=CN(N=N5)C(C=C6)=CC7=C6C(NCCCNCC8=CC=C9C(C=CN9)=C8)=CC=N7
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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 BET Degrader-14 Related Classifications
HY-179588 Related Classifications
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