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.
Kinase Assay
Cell Assay
Animal Administration
References
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