STING agonist-1 (G10)

For research use only.

Catalog No.S8954

STING agonist-1 (G10) Chemical Structure

CAS No. 702662-50-8

STING agonist-1 (G10) is a novel human-specific STING agonist that triggers IFN regulatory factor 3 (IRF3)/ type I interferon (IFN)-associated transcription in human fibroblasts. STING agonist-1 (G10) potently reduces growth of Chikungunya virus (CHIKV) with IC90 of 8.01 μM and blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) with IC90 of 24.57 μM.

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Biological Activity

Description STING agonist-1 (G10) is a novel human-specific STING agonist that triggers IFN regulatory factor 3 (IRF3)/ type I interferon (IFN)-associated transcription in human fibroblasts. STING agonist-1 (G10) potently reduces growth of Chikungunya virus (CHIKV) with IC90 of 8.01 μM and blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) with IC90 of 24.57 μM.
Targets
STING [1]
()
IRF3/IFN [1]
()
CHIKV [1]
(Cell-based assay)
VEEV [1]
(Cell-based assay)
8.01 μM 24.57 μM
In vitro

G10 induces IFN/IRF3- but not NF-κB-dependent transcription in human fibroblasts. G10 elicits antiviral activity against New and Old World Alphaviruses. G10 induces STING-dependent synthesis and secretion of bioactive interferon. G10 triggers IRF3-dependent activity and induces innate antiviral mRNA expression in primary human cells.[1]

In vivo

Because G10-induced innate immune activation is not observed in murine cells, DMXAA (an analogs of G10, with similar physiological effects) is used in the commenly used mice model of CHIKV infection. STING agonism inhibits CHIKV replication in vivo.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: Human foreskin fibroblasts, Vero cells, BHK-21 cells, C6/36 cells, RAW264.7 cells, THP1-ISG-Lucia cells, Human peripheral blood mononuclear cells
  • Concentrations: 6.25-200 μM, 100 μM
  • Incubation Time: 7 h, 18 h
  • Method:

    --


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 63 mg/mL (146.21 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 430.88
Formula

C21H16ClFN2O3S

CAS No. 702662-50-8
Storage powder
in solvent
Synonyms N/A
Smiles C1C(=O)N(C2=C(S1)C=CC(=C2)C(=O)NCC3=CC=CO3)CC4=C(C=CC=C4Cl)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00840008 Completed Other: Educational intervention Peptic Ulcer Hemorrhage McGill University Health Centre/Research Institute of the McGill University Health Centre|Horizon Health Network|Queen Elizabeth II Health Sciences Centre|St-Johns Health Sciences Centre|Centre hospitalier de l''Université de Montréal (CHUM)|Jewish General Hospital|Montreal General Hospital|Royal Victoria Hospital Canada|Maisonneuve-Rosemont Hospital|St Mary''s Hospital London|Centre Hospitalier Pierre Boucher|Cité de la Santé Hospital|Centre Hospitalier Anna Laberge|Hotel Dieu Hospital|CHAUQ - Hopital Saint Sacrement and Hopital Enfant Jesus|CISSS de Chaudière-Appalaches|Hamilton Health Sciences Corporation|Unity Health Toronto|Sunnybrook Health Sciences Centre|Toronto General Hospital|York Central Hospital Ontario|Lakeridge Health Corporation|Guelph General Hospital|London Health Sciences Centre|The Ottawa Hospital|Kingston Health Sciences Centre|Scarborough General Hospital|Matsqui-Sumas-Abbotsford General Hospital and Mission Memorial Hospital|Vancouver General Hospital|Peter Lougheed Centre/The Calgary General Hospital|Foothills Medical Centre|Rockyview General Hospital|Grey Nuns Hospital|University of Alberta|Royal Alexandra Hospital|Misericordia|Royal University Hospital Foundation|Regina General Hospital|University of Manitoba September 2008 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID