VGD020
VGD020 is a highly potent and selective Sec61 translocon inhibitor. VGD020 suppresses the expression of cell surface CD4 by inhibiting signal peptide-dependent co-translational ER translocation, interferes with the initiation of ER translocation of dengue virus polyprotein, and reduces the expression of Sortilin in breast cancer cells. VGD020 exhibits broad anti-flavivirus and anti-HIV activities. VGD020 can be used in research related to dengue virus infection, Zika virus infection, yellow fever virus infection, human immunodeficiency virus infection, and breast cancer.
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- CAS No.: 1322645-32-8
- 화학식: C31H45N3O5S2
- 분자량:603.84
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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
Biological Activity
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
0.15 μM
Compound: 1; VGD020
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Binding affinity to human CD4 signal peptide expressed in CHO cells assessed as down-modulation of YFP-fused CD4 expression after 24 hrs by flow cytometric analysis
Binding affinity to human CD4 signal peptide expressed in CHO cells assessed as down-modulation of YFP-fused CD4 expression after 24 hrs by flow cytometric analysis
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[PMID: 26974263] |
VGD020 (0.01-10 μM; 4-5 days) potently inhibits DENV2 replication in Vero cells, and achieves complete antiviral activity at micromolar concentrations[1].
VGD020 (0.01-100 μM; 4-5 days) exhibits low cytotoxicity in Vero cells, with minimal effects on cell viability even at concentrations as high as 100 μM[1].
VGD020 (0.01-10 μM; 4-5 days) potently inhibits DENV2 replication in Huh7 cells, and achieves complete antiviral activity at micromolar concentrations[1].
VGD020 (0.02-2 μM; 48 h) inhibits the expression of viral E protein in Huh7 cells infected with dengue virus type 2 (DENV2), and complete inhibition is achieved at a concentration of 0.4 μM after 48 h[1].
VGD020 (2 μM; 72 h) potently inhibits the expression of viral E protein in Huh7 cells infected with dengue virus type 2 (DENV2)[1].
VGD020 (1 μM; 0-24 h) exerts antiviral effects against DENV2 in Vero cells at the post-entry stage, and retains full activity even when added 8 h post-infection[1].
VGD020 (0.4-10 μM; 18 h) inhibits the expression of DENV2 prM and E proteins in transiently transfected HEK293T cells in a concentration-dependent manner, and its potency is consistent with its antiviral activity[1].
VGD020 (0.4-10 μM; 18 h) does not inhibit the expression of DENV2 NS1 protein in transiently transfected HEK293T cells even at concentrations as high as 10 μM[1].
VGD020 (0.4-10 μM; 18 h) selectively inhibits the expression of DENV2 prM protein, but does not inhibit the expression of E protein, in transiently transfected HEK293T cells[1].
VGD020 (0.15-15 μM) selectively inhibits Sec61-mediated co-translational translocation of DENV2 prM protein into the ER lumen in cell-free assays, with no effect on protein translation[1].
VGD020 (0.15-15 μM) does not inhibit Sec61-mediated co-translational translocation of truncated DENV2 E protein into the ER lumen in cell-free assays[1].
VGD020 (0.4-10 μM; 18 h) induces inhibition of DENV2 polyprotein trafficking, which in turn leads to proteasomal degradation of the precursor; co-treatment with MG132 partially reverses this effect in CHO-K1 cells[1].
VGD020 (0.01-10 μM; 18 h) potently inhibits the expression of 14C-prM62-VSV-G chimeric protein in HEK293T cells, with an IC50 of 308 nM[1].
VGD020 (0.01-10 μM; 18 h) does not inhibit the expression of M21-E62-VSV-G or E23-NS162-VSV-G chimeric proteins in HEK293T cells even at concentrations as high as 10 μM[1].
VGD020 (0.01-10 μM; 18 h) potently inhibits the expression of chimeric proteins containing the DENV2 C14 signal peptide sequence (the major determinant of sensitivity to VGD020), with an IC50 of 41 nM in HEK293T cells[1].
VGD020 (0.01-10 μM; 18 h) potently inhibits the expression of chimeric proteins containing C14 signal peptide sequences from multiple flaviviruses (DENV1, DENV3, DENV4, ZIKV) in HEK293T cells, with its IC50 value stably maintained at approximately 100 nM[1].
VGD020 (18 h) downregulates the expression of sortilin in HEK293T cells in a dose-dependent manner, with an IC50 of 0.5 μM[2].
VGD020 (24 h) potently downregulates CD4 expression in CHO CD4-YFP cells, with an IC50 of 46 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DENV2-infected Huh7 cells
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Concentration:0.02, 0.08, 0.4 and 2 μM
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Incubation Time:48 h
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Result:Completely suppressed cellular expression of viral E protein at 0.4 μM.
Showed partial inhibition of viral E protein expression at lower concentrations relative to untreated infected controls.
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Cell Line:transiently transfected HEK293T cells (with plasmid encoding DENV2 C14-prM-E)
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Concentration:0.4, 2 and 10 μM
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Incubation Time:18 h
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Result:Concentration-dependently inhibited expression of both prM and E proteins.
Achieved significant suppression at all tested concentrations relative to untreated transfected controls.
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Cell Line:transiently transfected HEK293T cells (with plasmid encoding DENV2 E23-NS1-V5)
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Concentration:0.4, 2 and 10 μM
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Incubation Time:18 h
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Result:Had no inhibitory effect on NS1 protein expression at concentrations up to 10 μM.
Resulted in NS1 expression levels comparable to untreated transfected controls.
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Cell Line:transiently transfected HEK293T cells (with plasmids encoding either DENV2 M21-E or C14-prM)
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Concentration:0.4, 2 and 10 μM
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Incubation Time:18 h
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Result:Concentration-dependently inhibited prM protein expression, with significant suppression at 2 and 10 μM.
Had no inhibitory effect on E protein expression at any tested concentration.
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Cell Line:transiently transfected CHO-K1 cells (with plasmid encoding DENV2 C14-prM-E_V5/FLAG/MYC)
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Concentration:0.4, 2 and 10 μM (alone or with 200 nM MG132)
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Incubation Time:18 h
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Result:Rescued a small amount of the uncleaved prM-E polyprotein precursor (75 kDa) when combined with MG132, which was not detected in VGD020-only or untreated samples.
Resulted in non-glycosylated precursor in combination treatment samples.
Chemical Information
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CAS No. 1322645-32-8
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분자량 603.84
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화학식 C31H45N3O5S2
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SMILES
O=S(C1=CC=C(C=C1)OC)(N2CC(CN(S(=O)(C3=CC=C(C)C=C3)=O)CCCN(CC4CCCCC4)CCC2)=C)=O
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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
[1].
Verhaegen M, et al. Sec61 translocon inhibitor flavitransin blocks selectively dengue virus polyprotein insertion in the ER with pan-orthoflavivirus antiviral potency. Cell Rep. 2025 Dec 23;44(12):116642.
[Content Brief]
[2]. Berger K, et al. Reduction of Progranulin-Induced Breast Cancer Stem Cell Propagation by Sortilin-Targeting Cyclotriazadisulfonamide (CADA) Compounds. J Med Chem. 2021;64(17):12865-12876. [Content Brief]
[3]. Demillo VG, et al. Unsymmetrical cyclotriazadisulfonamide (CADA) compounds as human CD4 receptor down-modulating agents. J Med Chem. 2011;54(16):5712-5721. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VGD020 Related Classifications
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