G10, STING signaling activator

STING agonist-1 (G10) is a novel human-specific STING agonist that elicits antiviral activity against emerging Alphaviruses. G10 potently blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) (IC90 = 24.57 μM). IC50 value: 24.57 μM (IC90)Target: VEEV, STINGin vitro: G10 does not bind to STING directly, however, G10 represents the first synthetic small molecule characterized as an indirect activator of human STING-dependent phenotypes.100 μM G10 (a concentration over twelve times the IC90 for CHIKV and over four times the IC90 for VEEV). G10 induces IFN/IRF3- but not NF-κB-dependent transcription in human fibroblasts. G10 Induces IFN/IRF3- but not NF-κB-Dependent Transcription in Human Fibroblasts. G10 activates IRF3, but not canonical NF-κB pathways in human fibroblasts. G10 elicits antiviral activity against New and Old World Alphaviruses. G10 stimulates phosphorylation of IFN regulatory factor 3 (IRF3) in a manner similar to that triggered by UV-inactivated cytomegalovirus (UV-CMV) and Sendai virus (SeV). G10 induces synthesis and secretion of bioactive type I and III IFNs and generates an antiviral state in fibroblast cells positive for STING, IRF3, and STAT1 proteins. G10 triggers innate immune responses that involve expression of IRF3-dependent genes including type I and III interferons.

Signaling Pathways >> Immunology/Inflammation >> STING

Research Areas >> Infection

[1]. Sali TM, et al. Characterization of a Novel Human-Specific STING Agonist that Elicits Antiviral Activity Against Emerging Alphaviruses. PLoS Pathog. 2015 Dec 8;11(12):e1005324.

CCCP | ADU-S100 ammonium salt | DMXAA (Vadimezan) | C 176 | Cyclic-di-GMP | cGAMP | STING agonist-1(compound 3)trihydrochloride