G10 (STING agonist-1)

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. 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.

G10 (STING agonist-1) Chemical Structure

G10 (STING agonist-1) Chemical Structure

CAS: 702662-50-8

Selleck's G10 (STING agonist-1) has been cited by 1 publication

Purity & Quality Control

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

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Biological Activity

Description 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. 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
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]

Cell Research 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

--

In Vivo
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]

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

Chemical Information & Solubility

Molecular Weight 430.88 Formula

C21H16ClFN2O3S

CAS No. 702662-50-8 SDF --
Smiles C1C(=O)N(C2=C(S1)C=CC(=C2)C(=O)NCC3=CC=CO3)CC4=C(C=CC=C4Cl)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 63 mg/mL ( (146.21 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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