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STING agonists and inhibitors act on an adaptor protein of the cytosolic DNA sensing pathway. Stimulator of interferon genes (STING) was described in 2008 as an endoplasmic reticulum adaptor needed for innate immune signaling and type I interferon induction. STING binds cyclic dinucleotides directly, both bacterial molecules such as cyclic di-GMP and the mammalian second messenger made by cyclic GMP-AMP synthase (cGAS) once it detects cytosolic DNA. Agonists listed here include 2',3'-cGAMP, Cyclic-di-GMP, ADU-S100 disodium salt (MIW815 disodium salt) and numbered compounds such as STING agonist-1. Inhibitors include H-151 and the mouse-directed C-176 and C-178, which belong to a class of covalent compounds that modify a cysteine of the transmembrane region.
Synonyms: G10
STING agonist-1 (G10) is a novel human-specific STING agonist that elicits antiviral activity against emerging Alphaviruses.
Synonyms: MIW 815; ADUS100
ADU-S100 (MIW815) is a synthetic cyclic dinucleotide (CDN) agonist (activator) of Stimulator of Interferon Genes (STING), a receptor crucial to activate the innate (endogenous) immune system.
STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM.
H-151 is a highly potent, selective and covalent antagonist of STING, reduces TBK1 phosphorylation and suppresses human STING palmitoylation.
Synonyms: c-di-GMP; cyclic diguanylate; 5GP-5GP
Cyclic-di-GMP is a STING agonist and a ubiquitous second messenger that regulates biofilm formation, motility, and virulence in diverse bacterial species.
STING agonist-3, compound 3, is a selective and non-nucleotide small-molecule STING agonist, which has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 nM for human PBMCs.
diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 for human PBMCs.
Synonyms: Cyclic diadenylate; Cyclic-di-AMP
c-di-AMP (Cyclic diadenylate) is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF.
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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.
MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity.
M04 is a potent agonist of stimulator of interferon genes (STING), specifically activating the wild-type human STING in HEK293T cells while demonstrating no efficacy with the HAQ STING variant or in mouse RAW 264.7 cells. It effectively induces the expression of pro-inflammatory cytokines such as TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At a concentration of 50 µM, M04 enhances dendritic cell maturation, promoting the expression of MHC class II (HLA-DR) and co-stimulatory molecules (CD40, CD80, CD86), thereby boosting T cell activation. This reagent is valuable for research in inflammatory immune diseases.
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STING Agonist-45 is a selective agonist of the stimulator of interferon genes (STING), exhibiting an EC50 value of 0.28 μM. It activates the innate immune response via the cGAS-STING pathway, leading to the upregulation of critical markers such as p-TBK1 and IRF3. STING Agonist-45 effectively stimulates the production of type I interferons, including IFN-β, as well as cytokines like TNF-α and IL-6 in human peripheral blood mononuclear cells (PBMCs). This compound shows potential in enhancing anti-tumor immunity, inhibiting tumor growth, and promoting CD8+ T cell infiltration in animal models, making it a valuable tool for research into STING-related diseases.
PDIC-NC is a STING agonist that promotes the activation of the STING pathway, leading to enhanced immune responses against tumors. This compound is cytotoxic to tumor cells and induces reactive oxygen species (ROS) production, as well as apoptosis and autophagy. With its specific distribution to lung tissue, PDIC-NC is particularly valuable for research applications focused on lung cancer.
STING Agonist-50 is a potent oral STING agonist that activates the STING signaling pathway with an IC50 of 3.457 μM. It facilitates the phosphorylation of downstream proteins TBK1 and IRF3, leading to the enhanced expression of key cytokines such as IFN-β, CXCL10, and IL-6. This compound has demonstrated the ability to inhibit tumor growth in syngeneic mouse models, making it a valuable tool for research focused on colorectal cancer.
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STING agonist-18 is a potent agonist of the stimulator of interferon genes (STING) pathway, known for its ability to activate immune responses. This compound is particularly useful in the synthesis of antibody-drug conjugates (ADCs), such as Trastuzumab conjugates, facilitating targeted therapeutic approaches. Its application in cancer immunotherapy and related research enhances the understanding of STING pathway modulation in tumor microenvironments.
Synonyms: Cyclic diadenylate disodium; Cyclic-di-AMP disodium
c-di-AMP disodium is a cyclic dinucleotide serving as a STING agonist, which interacts with the STING protein to activate the TBK1-IRF3 signaling pathway. This activation leads to the production of type I interferons and tumor necrosis factor, playing a pivotal role in the immune response. In addition to its function in immune modulation, c-di-AMP is a bacterial second messenger that regulates various physiological processes in Gram-positive bacteria, including growth and virulence. Its properties also make it an effective mucosal adjuvant for enhancing both humoral and cellular immune responses in research applications.
STING Agonist-30 is a potent agonist that activates the Stimulator of Interferon Genes (STING) pathway. This compound elicits a robust immune response and enhances STING-dependent immune activation. It demonstrates significant antiviral activity against a range of viruses, including herpes simplex virus (HSV), rotavirus, and severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), making it valuable for research in antiviral therapies and immune modulation.
diABZI-V/C-DBCO is a potent STING agonist with an EC50 of 1.47 nM. It activates the STING pathway to promote the production of type I interferons, particularly IFN-β, enhancing immune responses. This compound acts as a substrate for cathepsin B, leading to the release of active diABZI-amine through cathepsin B-mediated cleavage. In preclinical studies using an orthotopic mouse model of breast cancer, diABZI-V/C-DBCO has been shown to elevate serum levels of IFN-β and increase the frequency of granzyme B+ CD8+ T cells, making it valuable for research in triple-negative breast cancer.
SNX281 is a selective STING agonist that functions by inducing homodimerization at the STING binding site, leading to a conformational shift that activates STING and initiates downstream signaling pathways. This compound effectively stimulates the production of type I interferons, including IFN-β, as well as TNF-α and IL-6, resulting in enhanced T cell responses and prolonged immune memory. SNX281 demonstrates anti-tumor activity and is valuable for research applications in colorectal cancer, melanoma, advanced solid tumors, lymphoma, and ovarian cancer.
Synonyms: c-di-GMP disodium; cyclic diguanylate disodium; 5GP-5GP disodium
Cyclic-di-GMP disodium functions as a STING agonist and serves as a crucial bacterial second messenger. It orchestrates various bacterial behaviors such as motility, virulence, biofilm formation, and cell cycle regulation. Additionally, cyclic-di-GMP disodium exhibits anti-cancer activity by inhibiting cell proliferation and promoting CD4 receptor expression along with inducing cell cycle arrest. This compound is valuable for applications in cancer research.
STING agonist-12 (Compound 53) is a potent agonist that activates the human stimulator of interferon genes (STING) pathway, exhibiting an EC50 value of 185 nM. This compound serves as a valuable tool for immunological research, particularly in studying innate immune responses and antitumor immunity. Its ability to modulate STING activity makes it a promising candidate for assessing therapeutic strategies in cancer and infectious diseases.
STING agonist-20 is a potent agonist of the STING pathway, which plays a critical role in the innate immune response. This compound is utilized in the synthesis of XMT-2056, serving as an important tool in cancer research and the investigation of inflammatory and immune-related diseases. Its application as a vaccine adjuvant allows for enhanced immune activation, making it a valuable reagent in immunotherapy studies.
STING Agonist-22 (CF501) is a potent non-nucleotide agonist targeting the stimulator of interferon genes (STING). This compound effectively activates STING to induce a type I interferon (IFN-I) response and drive the production of proinflammatory cytokines. STING Agonist-22 serves as an adjuvant to enhance protein vaccine efficacy, promoting robust and sustained immune protection. It is particularly relevant for research on SARS-CoV-2 variants and related sarbecovirus diseases.
STING antagonist-1 is a selective antagonist of the Stimulator of Interferon Genes (STING) pathway, exhibiting an IC50 of 3.8 nM. This compound is valuable for research applications related to autoimmune and inflammatory diseases, allowing for the investigation of STING-mediated cellular responses and therapeutic interventions.
