FC-14367
FC-14367 is a PROTAC degrader targeting the HIV-1 Nef protein. FC-14367 forms a ternary complex between HIV-1 Nef and CRBN, inducing ubiquitination and proteolytic degradation of Nef. FC-14367 restores the expression of CD4 and MHC-I on the cell surface and inhibits Nef-dependent enhancement of HIV-1 replication. FC-14367 can be used in studies related to HIV-1 infection.
(Pink: Target protein ligand; Blue: Cereblon ligand (HY-138793); Black: linker (HY-W015967)).
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- No. CAS: 3066893-65-7
- Fòrmula: C38H35ClFN7O6
- Peso molecular:740.18
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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HIV-1 Nef |
FC-14367 (90 s association phase, 180 s dissociation phase) binds to diverse M-group HIV-1 Nef variants, SIV Nefmac239, and the human Cereblon Thalidomide (HY-14658)-binding domain with nanomolar affinity[1].
FC-14367 (10 μM; 24 h) significantly induces ubiquitylation of HIV-1 Nef in 293T cells at 10 μM[1].
FC-14367 (3 μM; 48 h) reduces HIV-1 Nef protein levels in CEM/Nef-eGFP T cells to ~65% of control levels after 48 h of incubation[1].
FC-14367 (1 μM; 4 days) suppresses wild-type HIV-1 NL4-3 replication in activated donor PBMCs at 1 μM to levels equivalent to the Nef-defective mutant, while maintaining near-100% cell viability relative to DMSO controls[1].
FC-14367 (3 μM; 24 h) induces degradation of HIV-1 Nef-eGFP in CEM/Nef-eGFP T cells, restoring cell-surface CD4 and MHC-I expression to ~75% and ~60% of control levels, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Doxycycline-inducible CEM/Nef-eGFP T cells
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Concentration:3 μM
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Incubation Time:48 h
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Result:Reduced Nef protein levels to ~65% of DMSO control levels, as measured by Nef-to-Actin band intensity ratios.
Chemical Information
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No. CAS 3066893-65-7
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Peso molecular 740.18
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Fòrmula C38H35ClFN7O6
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SMILES
O=C1NC(C(CC1)N2C(C3=C(C2)C(OCC(N4CCC(CC4)C5=NN(C6=NC7=C(N6)C=CC(Cl)=C7)C(O)=C5CCC8=CC=C(C=C8)F)=O)=CC=C3)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)