Jun15702
Jun15702 is a PROTAC degrader targeting the capsid protein VP1 of enterovirus D68. Jun15702 recruits the Cereblon (CRBN) E3 ligase and activates the ubiquitin-proteasome pathway. Jun15702 inhibits viral entry and exerts inhibitory effects during the early, middle and late stages of viral replication. Jun15702 exhibits antiviral activity against multiple wild-type enterovirus D68 strains, and also shows submicromolar antiviral activity against the Pleconaril (HY-19952)-resistant enterovirus D68 variant rMO-VP1 F159V. Jun15702 can be used in studies related to enterovirus D68 (EV-D68) infection.
(Pink: Enterovirus ligand (HY-183010); Blue: Cereblon ligand (HY-183011); Black: linker).
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- Formule: C47H54F3N7O11
- Masse moléculaire:949.97
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
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Cereblon |
Jun15702 (10 μM; 0-8 h) depletes VP1 levels in EV-D68 US/MO/14-18947-infected RD cells when added before, during, or after viral entry, and effectively degrades the pleconaril-resistant VP1F159V mutant protein[1].
Jun15702 (0.3-30 μM; 2-10 h) induces dose-dependent, CRBN-mediated degradation of VP1 protein in EV-D68 US/MO/14-18947-infected RD cells, as confirmed by Western blot analysis[1].
Jun15702 (range; 60 h) has a CC50 of 81.8 μM in RD cells, showing no significant cytotoxicity at concentrations below 50 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EV-D68 US/MO/14-18947-infected RD cells, rMO-VP1 F159V EV-D68-infected RD cells
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Concentration:10 μM
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Incubation Time:-1-8 h, 0-8 h, 1-8 h, 2-8 h, 3-8 h, 4-8 h, 5-8 h, 6-8 h, 7-8 h (relative to infection; wild-type testing); 2-8 hpi (mutant strain testing)
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Result:Nearly completely depleted VP1 levels when added before or during viral entry (-1-8 h, 0-8 h).
Retained potent inhibitory activity when added post-entry (2-8 h, 3-8 h, 4-8 h, 5-8 hpi), only gradually losing activity at 6-8 h and 7-8 hpi.
Dramatically reduced VP1 immunofluorescence signals when added at 2-8 hpi to rMO-VP1 F159V-infected cells, whereas pleconaril showed no inhibition.
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Cell Line:EV-D68 US/MO/14-18947-infected RD cells
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Concentration:0, 0.3, 1, 3, 10, 30 μM; 10 μM lenalidomide-5-Br combined with increasing concentrations of Jun15702
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Incubation Time:2-10 hpi
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Result:Caused a dose-dependent reduction in VP1 protein levels, whereas pleconaril and lenalidomide-5-Br did not induce VP1 degradation.
Preserved VP1 degradation at concentrations above 3 μM when combined with 10 μM lenalidomide-5-Br.
Chemical Information
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Masse moléculaire 949.97
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Formule C47H54F3N7O11
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SMILES
O=C(NCCCOCCOCCOCCCNC(C1=NOC(CCCOC2=C(C=C(C=C2C)C3=NOC(C(F)(F)F)=N3)C)=C1)=O)CCCC#CC4=CC=C(CN(C5CCC(NC5=O)=O)C6=O)C6=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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