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G10 (STING agonist-1) STING agonist

Cat.No.S8954

G10 (STING agonist-1) is a novel human-specific STING agonist that triggers IFN regulatory factor 3 (IRF3)/ type I interferon (IFN)-associated transcription in human fibroblasts. This compound 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.
G10 (STING agonist-1) STING agonist Chemical Structure

Chemical Structure

Molecular Weight: 430.88

Quality Control

Batch: S895401 DMSO]63 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.92%
99.92

Chemical Information, Storage & Stability

Molecular Weight 430.88 Formula

C21H16ClFN2O3S

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 702662-50-8 -- Storage of Stock Solutions

Synonyms N/A Smiles C1C(=O)N(C2=C(S1)C=CC(=C2)C(=O)NCC3=CC=CO3)CC4=C(C=CC=C4Cl)F

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (146.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Mechanism of Action

Targets/IC50/Ki
STING [1]
IRF3/IFN [1]
CHIKV [1]
(Cell-based assay)
8.01 μM
VEEV [1]
(Cell-based assay)
24.57 μM
In vitro

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

In vivo

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

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00840008 Completed
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|Queen''s University|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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