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)).
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- 화학식: C37H33F3N6O9
- 분자량:762.69
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보관:
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
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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.
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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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분자량 762.69
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GNF-2-deg Related Classifications
HY-161804 Related Classifications
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