STING

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-176 is a strong and covalent mouse STING inhibitor.

STING-IN-17 is a potent inhibitor of STING (Stimulator of Interferon Genes), with human STING IC50 of 29 nM and mouse STING IC50 of 15 nM. This compound effectively inhibits the phosphorylation of STING, TBK1, and IRF3, leading to a dose-dependent reduction in the mRNA expression of key inflammatory markers such as IP10, IFNB1, and ISG56. STING-IN-17 also decreases reactive oxygen species (ROS) levels and inhibits the activation of apoptosis-related proteins cleaved-PARP and caspase-3. Its potential applications make it valuable for research into inflammatory conditions, particularly acute kidney injury.

STING-IN-16 is a potent inhibitor of the Stimulator of Interferon Genes (STING) pathway, exhibiting IC50 values of 44 nM in human cells and 32 nM in murine cells. It effectively inhibits STING activation, leading to restoration of renal mitochondrial function, reduction of reactive oxygen species (ROS) production, and decreased cell apoptosis. With demonstrated anti-inflammatory efficacy in vivo, STING-IN-16 is valuable for research focused on autoimmune and autoinflammatory diseases.

STING-IN-11 is a potent STING inhibitor with an IC50 of 37.8 nM. By blocking the palmitoylation of the STING protein, it effectively inhibits STING-mediated downstream signaling and associated inflammatory pathways. This compound demonstrates favorable in vivo safety, making it an excellent candidate for research into STING-related inflammatory and autoimmune diseases.

SN-011 is a selective inhibitor of the STING pathway, displaying an IC50 of 76 nM. By competing with cyclic dinucleotides (CDNs) for the binding site on the STING dimer, SN-011 effectively prevents CDN binding and subsequent STING activation. This compound is valuable for investigating STING-mediated autoimmune and inflammatory diseases, offering insights into therapeutic strategies targeting this critical signaling pathway.

STING-IN-2 is a potent covalent inhibitor of Stimulator of Interferon Genes (STING), effectively targeting both mouse and human STING isoforms. This compound is instrumental in studying the role of STING in autoinflammatory diseases, facilitating the exploration of therapeutic interventions. Its ability to modulate STING activity makes it a valuable tool for researchers investigating immune response and signaling pathways.

LB244 is a STING inhibitor that functions by modulating the STING signaling pathway to reduce inflammation. It exhibits a potent inhibitory effect (EC50 = 0.8 μM) on STING-dependent inflammatory responses. While LB244 shows promising potential in preclinical studies, its pharmacokinetic profile suggests limited oral bioavailability in murine models. This compound is suitable for research applications focused on understanding STING-related inflammatory disorders.

STING-IN-3 is a potent inhibitor of the stimulator of interferon genes (STING), specifically targeting both human and murine STING. It covalently modifies the conserved transmembrane cysteine residue at position 91, effectively preventing activation-induced palmitoylation. This activity provides valuable utility in research applications exploring STING-related pathways in immune response and therapeutic interventions in autoimmune diseases and cancer.

SN-001 is a selective inhibitor of the STING (Stimulator of Interferon Genes) pathway, exhibiting an IC50 of 3.82 μM. This compound is valuable for investigating the role of STING in immune responses and inflammatory diseases. Its inhibitory activity allows for the evaluation of STING's effects on cytokine production and other immune-related pathways, making it a useful tool for research in immunology and drug development.

STING-IN-4 is a potent STING inhibitor that effectively reduces the expression and activation of STING and nuclear factor-κB (NF-κB) signaling pathways. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for investigating sepsis and related inflammatory conditions. Researchers can utilize STING-IN-4 to explore the therapeutic potential of modulating STING activity in various biological contexts.

STING-IN-7 is a potent inhibitor of the Stimulator of Interferon Genes (STING) pathway, demonstrating an IC50 of 11.5 nM. This compound effectively inhibits the phosphorylation of STING, interferon regulatory factor 3 (IRF3), and TANK-binding kinase 1 (TBK1). STING-IN-7 is valuable for investigating the role of STING modulation in autoimmune and inflammatory disease research.

STING-IN-15 is a potent STING inhibitor that exhibits an IC50 of 116 nM against human STING and 96.3 nM against mouse STING. It effectively disrupts the STING signaling pathway in cellular models, leading to a decrease in the secretion of IFN-β and IP-10, and downregulating the expression of key inflammatory markers such as ISG15, ISG56, and TNF-α. Additionally, STING-IN-15 shows promise in reducing systemic and renal inflammation triggered by STING agonists in murine models, thereby mitigating tissue damage and the overexpression of interferon-related genes. This compound is valuable for research into acute kidney injury and various autoimmune/inflammatory diseases.

H-151 Alkyne is a selective inhibitor of STING (Stimulator of Interferon Genes). This compound demonstrates potential for modulating immune responses, making it valuable in the study of autoimmune diseases such as systemic lupus erythematosus and scleroderma, as well as autoinflammatory conditions. Its ability to interfere with STING pathways allows researchers to explore therapeutic strategies targeting these diseases.

STING-IN-5 is a potent inhibitor of the STING pathway, specifically targeting the STING protein to attenuate LPS-induced nitric oxide synthesis in macrophages, with an IC50 value of 1.15 μM. This compound effectively reduces inflammatory responses, making it valuable for research focused on anti-inflammatory diseases and sepsis. Its ability to modulate immune responses highlights its potential in elucidating the role of STING in various pathological contexts.

STING-IN-14 is a potent STING inhibitor with an IC50 value of 0.6 nM. This compound effectively suppresses the activation of the IRF pathway in THP1-DualTM cells, making it a valuable tool for studying the role of STING in immune responses. STING-IN-14 is particularly relevant for research focused on autoimmune diseases, contributing to a better understanding of disease mechanisms and potential therapeutic interventions.

STING modulator-3 is a selective STING inhibitor that targets the R232 variant of STING, exhibiting an inhibition constant (Ki) of 43.1 nM in scintillation proximity assays. This compound does not influence IRF-3 activation or TNF-β induction in THP-1 cells, making it a valuable tool for studying STING-mediated signaling pathways and their implications in immune responses and inflammatory diseases. Its specificity and potency provide researchers with a resource for exploring STING-related mechanisms in various biological contexts.