sting agonist 1

STING agonist-1 (G10) is a human-specific agent that elicits antiviral activity against emerging Alphaviruses.

diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

diABZI STING agonist-1 (trihydrochloride) is a stimulator of interferon genes (STING) receptor agonist.

diABZI STING agonist-1 is a selective and potent interferon gene-stimulating receptor (STING) agonist with potential antitumor and anti-inflammatory activity for the study of cancer.

STING agonist 12b is an agonist of stimulator of interferon genes (STING).1It binds to STING (Kd= 26.4 μM) and induces interferon reporter gene expression in cells expressing human or mouse STING (EC50s = 7.45 and 10.23 μM, respectively). STING agonist 12b (40 μM) induces expression of TNF-a, IL-6, IP-10, and IL-1b in THP-1 cells. 1.Hou, S., Lan, X.-j., Li, W., et al.Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonistsBioorg. Chem.95103556(2020)

STING agonist 1a is an agonist of stimulator of interferon genes (STING).1It induces expression of an IRF-inducible SEAP reporter gene in a cell-based assay (EC50= 16.77 μM). STING agonist 1a (12.5-100 μM) induces expression of IFN-β, IL-6, and chemokine (C-X-C motif) ligand 10 (CXCL10) in THP-1 cells, an effect that can be reversed by STING knockout or the STING inhibitor H-151 . 1.Hou, H., Yang, R., Liu, X., et al.Discovery of triazoloquinoxaline as novel STING agonists via structure-based virtual screeningBioorg. Chem.100103958(2020)

STING agonist 12L is a stimulator of interferon genes (STING) agonist that exhibits binding affinity for both wild-type STING and its variants R232, AQ, and Q with half-maximal inhibitory concentrations (IC50s) of 1.15 µM for wild-type, 1.06 µM for R232, 0.61 µM for AQ, and 1.12 µM for Q. It effectively induces reporter gene expression in THP-1 and RAW 264.7 cells, with half-maximal effective concentrations (EC50s) of 0.38 µM and 12.94 µM, respectively. At a concentration of 5 µM, STING agonist 12L escalates the expression of IFNB1, CXCL10, and IL6 mRNA in THP-1 cells. When administered in vivo at a dose of 10 mg/kg, it enhances plasma IFN-β levels and considerably reduces tumor volume and the number of lung metastases in a B16/F10 murine melanoma model.

MSA-2 is an orally available non-nucleotide STING agonist. The non-covalent dimer of MSA-2 binds to STING with nanomolar affinity. It shows anti-tumor activity in syngeneic mouse tumor models, synergizes with anti-PD-1, stimulates tumor secretion of interferon-β, induces tumor regression, and has long-lasting anti-tumor immunity. [3]

STING agonist-3 trihydrochloride is a selective and non-nucleotide agonist of small-molecule STING(pEC50 and pEC50 of 7.5 and 9.5, respectively), has durable anti-tumor effect and tremendous potential to improve treatment of cancer.

CAY10748 is an agonist of stimulator of interferon genes (STING; IC50= 0.3794 μM in a competition binding assay).1It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC50s = 0.287 and >100 μM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β and the levels of chemokine (C-X-C motif) ligand 10 (CXCL10), and IL-6 in peripheral blood mononuclear cells (PBMCs) when used at a concentration of 10 μM. It also reduces tumor growth in a CT26 murine colon cancer model when administered at a dose of 0.15, but not 1.5, mg/kg. 1.Xi, Q., Wang, M., Jia, W., et al.Design, synthesis, and biological evaluation of amidobenzimidazole derivatives as stimulator of interferon genes (STING) receptor agonistsJ. Med. Chem.63(1)260-282(2019)

MSA-2 dimer, a selective and orally active non-nucleotide STING agonist with a dissociation constant (Kd) of 145 μM, demonstrates prolonged antitumor and immunogenic activity. It non-covalently binds to STING as a dimer, showing greater permeability compared to cyclic dinucleotide[1].

STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses grown in THF cells (EC90s = 16.44, 16.7, 18.84, 25.19, and 22.57 μM, respectively), an effect that is dependent on the presence of STING and the IFN-α/β receptor (IFNAR).References1. Gall, B., Pryke, K., Abraham, J., et al. Emerging alphaviruses are sensitive to cellular states induced by a novel small-molecule agonist of the STING pathway. J. Virol. 92(6), e01913-01917 (2018). STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses grown in THF cells (EC90s = 16.44, 16.7, 18.84, 25.19, and 22.57 μM, respectively), an effect that is dependent on the presence of STING and the IFN-α/β receptor (IFNAR). References1. Gall, B., Pryke, K., Abraham, J., et al. Emerging alphaviruses are sensitive to cellular states induced by a novel small-molecule agonist of the STING pathway. J. Virol. 92(6), e01913-01917 (2018).

STING agonist-7 is an agonist of non-nucleotide STING that binds selectively to mouse STING but not human STING [1].

BSP16 is a highly potent and orally active STING agonist, capable of selectively stimulating the interferon genes pathway. This compound, BSP16, holds great potential for cancer research [1].

Cyclic diadenylate (c-di-AMP) sodium functions as a STING agonist by binding to the STING transmembrane protein, thus activating the TBK3-IRF3 signaling pathway. This activation prompts the production of type I IFN and TNF. Additionally, c-di-AMP sodium serves as a bacterial second messenger in Gram-positive bacteria, where it plays crucial roles in regulating cell growth, survival, and virulence, as well as the host immune response. It also acts as a potent mucosal adjuvant by stimulating both humoral and cellular responses [1] [2] [3] [4].

IACS-8803 Disodium, a potent cyclic dinucleotide STING agonist, exhibits strong systemic antitumor efficacy [1].

IACS-8803 diammonium, a potent cyclic dinucleotide STING agonist, demonstrates robust systemic antitumor efficacy [1].

STING agonist-17 (compound 4a) is a highly potent stimulator of the STING pathway with an IC50 of 0.062 nM, demonstrating significant anti-cancer properties by promoting tumor immunization [1].

STING Agonist-13, a stimulator of interferon genes (STING) agonist, enhances cancer immunity through STING-mediated immune activation. It activates STING downstream signaling to promote type I interferon immune responses, significantly reduces tumor volume, and exhibits immunological memory-derived cancer inhibition [1].

STING Agonist-9 (Compound 45) is a powerful stimulator of the STING pathway, demonstrating potent activity with an EC50 of 1.2 nM against human STING (h-STING) and 32.82 μM against mouse STING (m-STING). It exhibits antitumor activity [1].

STING agonist-20-Ala-amide-PEG2-C2-NH2, an active scaffolding molecule, engages the stimulator of interferon genes (STING) pathway and is used in the synthesis of immune-stimulating antibody conjugates (ISAC), particularly in cancer research [1].

STING Agonist-20-Ala-amide-PEG2-C2-NH2 (Compound 30b) TFA, an active compound that interacts with the stimulator of interferon genes (STING), is utilized in the synthesis of immune-stimulating antibody conjugates (ISAC). This compound is also employed in cancer research [1].

CL845, a STING (stimulator of interferon genes) agonist analog to CL656, is instrumental in synthesizing conjugatable PRR (pattern recognition receptor) ligands aimed at targeting STING. It holds potential applications in researching cancers, immunological disorders, or infections [1].

Dazostinag (TAK-676 free base) is a stimulator of interferon genes (STING) protein agonist with antineoplastic properties and serves as a payload for the synthesis of antibody-drug conjugates (ADCs) [1] [2].