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.
STING agonist-3 is a selective small-molecule STING agonist. STING agonist-3 is a non-nucleotide STING agonist which has durable anti-tumor effect and tremendous potential to improve treatment of cancer[1].
ADU-S100 is an inducer of STING (stimulator of interferon genes). ADU-S100 has enhanced binding affinity to STING and activate all known human STING alleles.
Ulevostinag (MK-1454) is a STING agonist[1][2].
MSA-2 is an orally available non-nucleotide STING agonist, with EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 shows antitumor activity and stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models[1].
Cyclic-di-GMP is a STING agonist and a ubiquitous second messenger that regulates biofilm formation, motility, and virulence in diverse bacterial species.
STING-IN-6 (compound 50) is a potent STING inhibitor with a pIC50 of 8.9. STING-IN-6 has the potential for immunity research[1].
Vadimezan (ASA-404; DMXAA), the vascular disrupting agent, is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines.
Cyclic di-GMP (c-di-GMP) diammonium is a STING activator and a global bacterial second messenger, which regulates biofilm formation, motility, and virulence in diverse bacterial species[1][2].
diABZI STING agonist-1 (Tautomerism) is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 for human PBMCs.
diABZI-C2-NH2, an active analogue containing a primary amine functionality, is a STING agonist[1].
Cyclic di-GMP (c-di-GMP) disodium is a STING activator and a global bacterial second messenger, which regulates biofilm formation, motility, and virulence in diverse bacterial species[1][2].
STING agonist-34 (Compound 12L) is a potent STING agonist with an IC50 value of 1.15 μM and an EC50 of 0.38 μM in THP1 cells. STING agonist-34 could be used in cancer research[1].
SN-001 is a STING inhibitor with an IC50 of 3.82 μM[1].
2',3'-cGAMP-C2-PPA (45), A cyclic di-nucleotide, is a STING agonist (US20210015941A1). 2',3'-cGAMP-C2-PPA is a drug-linker conjugate for ADC that can be used in synthesis of antibody-drug conjugates for the targeted treatment of cancer[1].
SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity[1].
SN-011 is a potent and selective mouse and human STING inhibitor, with an IC50 of 76 nM for STING signaling. SN-011 competes with cyclic dinucleotide (CDN) for the binding pocket of the STING dimer, blocking CDN binding and STING activation. SN-011 can be used for the research of STING-driven autoimmune and inflammatory disease[1].
cGAMP(Cyclic GMP-AMP) is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA; STING ligand.Target:in vitro: cGAMP induced IFNβ RNA robustly even at concentrations as low as 10 nM. cGAMP was much more potent than c-di-GMP in inducing IFNβ based on ELISA assays. cGAMP was also more potent than c-di-GMP and c-di-AMP in activating IRF3. cGAMP binds to and activates STING to trigger the downstream signaling cascades [1]. On stimulation with cGAMP, fibroblasts from the patients showed increased transcription of IFNB1 but not of the genes encoding interleukin-1 (IL1), interleukin-6 (IL6), or tumor necrosis factor (TNF) [3]. cGAMP activates the endoplasmic reticulum (ER)-resident receptor STING, thereby inducing an antiviral state and the secretion of type I IFNs [4].in vivo: cGAMP can enhance the adaptive immune response to the model antigen ovalbumin in mice. cGAMP promotes antigen specific IgG and a balanced Th1/Th2 lymphocyte response in immunized mice [2].
STING agonist-31 is a STING agonist, with EC50 values of 0.24 and 39.51 μM for h-STING and m-STING. STING agonist-31 has antitumor efficiency[1].
STING modulator-3 is a STING inhibitor. STING modulator-3 inhibits R232 STING with an Ki value of 43.1 nM in scintillation proximity assay. STING modulator-3 has no effect on IRF-3 activation or TNF-β induction in THP-1 cells[1].
C-178, a covalent inhibitor of STING, binds to Cys91, potently and selectively suppresses the STING responses elicited by distinct bona fide activators in mouse but not human. C-178 significantly reduces STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity. C-178 blocks palmitoylation (PMA)-induced clustering of STING; inhibits the CMA-induced phosphorylation of TBK1 (downstream protein kinase of STING)[1].
STING modulator-5 (compound 38) is a STING modulator with a pIC50 value of 9.5. STING modulator-5 antagonizes peripheral blood mononuclear cells (PBMC) with a pIC50 value of 8.1. STING modulator-5 is a antagonist of THP-1 cells, it can be used for immunological disease research[1].
STING agonist-12 (Compound 53) is a potent, orally active human STING activator with an EC50 of 185 nM[1].
CL656 is an activator of stimulator of interferon genes (STING).
Antitumor agent-114 is a potent stimulator of interferon genes (STING) agonist. Antitumor agent-114 activates immunity and reduces tumor volume in a mouse model of breast cancer. Antitumor agent-114 can be used for immunity and cancer diseases research[1].
Ulevostinag isomer 1 (MK-1454 isomer 1) is the isomer of Ulevostinag. Ulevostinag is a STING agonist[1].
STING agonist-23 (CF502) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains[1].
STING modulator-4 (compound AIH05) is a competitive STING modulator with a Ki of 0.0933 μM for R232H STING. STING modulator-4 has an EC50 of >10 μM for p-IRF3 in THP-1 cell[1].
STING agonist-24 (CF504) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains[1].
SN-008, a less active SN-011 analog, can be used as a negative control[1].