GNF-2-deg
GNF-2-deg is a PROTAC degrader targeting the dengue virus envelope protein (DENV E protein), with a DC50 of 0.83 μM in Huh7.5 cells. GNF-2-deg induces CRBN- and proteasome-dependent proteolysis of intracellular E protein. GNF-2-deg inhibits E protein-mediated membrane fusion and blocks viral particle production. GNF-2-deg reduces viral yield in infected cells and retains activity against E protein βOG pocket mutant virus-like particles (VLP). GNF-2-deg can be used in the research of dengue virus infection, Zika virus infection, Japanese encephalitis, West Nile virus infection and yellow fever.
(Pink: Dengue Virus ligand (HY-11007); Blue: Cereblon ligand (HY-23095); Black: linker (HY-42149)).
For research use only. We do not sell to patients.
- Formula: C37H33F3N6O9
- Molecular Weight:762.69
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
Description
In Vitro
GNF-2-deg (0.07-20 μM; 24 h) induces CRBN- and proteasome-dependent intracellular degradation of DENV2 E protein in wild-type Huh7.5 cells, with a DC50 of 0.83 μM and a maximum degradation rate of 99%[1].
GNF-2-deg (0.01-100 μM; 24 h) exhibits CRBN-dependent enhanced anti-DENV2 activity in wild-type Huh7.5 cells, with an EC90 of 3.50 μM[1].
GNF-2-deg (3.5 μM; 24 h starting 4 h post-transfection) inhibits DENV2 VLP production in wild-type Huh7.5 cells via a CRBN-dependent mechanism[1].
GNF-2-deg (0.01-100 μM; 24 h) exhibits broad-spectrum and potent antiviral activity against mosquito-borne flaviviruses (ZIKV, JEV, West Nile virus Kunjin strain, YFV) in Huh7.5 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:wild-type and CRBN-deficient Huh7.5 cells
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Concentration:0.07, 0.15, 0.3, 0.6, 1.2, 2.5, 5, 10, 20 μM; 5 μM lenalidomide (24 h co-treatment); 0.5 μM MLN4924 (HY-70062) (24 h co-treatment); 2.5 μM MG-132 (HY-13259) (final 3 h co-treatment)
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Incubation Time:24 h; 3 h (MG-132 co-treatment)
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Result:Caused a concentration-dependent reduction in intracellular DENV2 E protein, with a DC50 of 0.83 μM and a maximum degradation (DCₘₐₓ) of 99%.
Was blocked by co-treatment with lenalidomide, MLN4924, or MG-132.
Showed no degradation of E in CRBN-deficient Huh7.5 cells or with the negative control compound GNF-2-deg-BUMP.
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Cell Line:wild-type and CRBN-deficient Huh7.5 cells
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Concentration:3.5 μM
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Incubation Time:24 h (starting 4 h post-transfection)
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Result:Reduced intracellular E protein abundance and secreted VLP levels to 18% and 24% of DMSO-treated controls, respectively, in wild-type Huh7.5 cells.
Lost activity in CRBN-deficient cells.
Retained activity comparable to wild-type VLPs against VLPs with single βOG pocket mutations (E-F193L, E-M196V, E-F279S).
Completely lost activity against the E-F193L/M196V double mutant.
Chemical Information
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Molecular Weight 762.69
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Formula C37H33F3N6O9
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SMILES
O=C(NCCOCCOCCOC1=CC=C2C(C(N(C3CCC(NC3=O)=O)C2=O)=O)=C1)C4=CC=CC(C5=CC(NC6=CC=C(OC(F)(F)F)C=C6)=NC=N5)=C4
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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.
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GNF-2-deg Related Classifications
HY-161804 Related Classifications
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