autoinflammatory

H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo.

STING-IN-2 (C-170) is a potent, covalent inhibitor of STING, effectively targeting both mouse (mmSTING) and human STING (hsSTING), and is applicable for autoinflammatory disease research.

RIP2 kinase inhibitor 1 is a potent and selective receptor interacting inhibitor of protein 2 (RIP2) kinase(RIP2 FP with an IC50 of 0.03 μM ),and is used for autoinflammatory disorders.

STING-IN-16 is an inhibitor of STING, with an IC50 value of 44 nM in humans and 32 nM in mice. This compound effectively suppresses the activation of the STING pathway in both human and mouse cells. STING-IN-16 aids in restoring kidney mitochondrial function, inhibits the production of reactive oxygen species (ROS), and reduces apoptosis. It exhibits significant anti-inflammatory effects in vivo and is a valuable tool for researching autoimmune and autoinflammatory diseases.

BMS-025 is an orthogonal STING agonist that can induce chemical shifts in the STINGM271 residue, thereby further activating STINGIFN signal transduction. BMS-025 is applicable in the study of monogenic autoinflammatory diseases such as SAVI.

diABZI-a1 is an orthogonal STING agonist with an EC50 of 117 nM for inducing IFNβ in human PBMCs. This compound is applicable in the study of monogenic autoinflammatory diseases such as SAVI disease.

MRT-3486 (Compound 5) is a cereblon-based molecular glue degrader for NEK7. It is suitable for research on autoinflammatory diseases.

diABZI-i functions as an orthogonal STING inhibitor, significantly suppressing cGAMP-induced IFNβ in PBMCs with an IC50 of 49 nM. Additionally, diABZI-i activates V155M SAVI constitutive signaling in a STINGV155M THP-1 cell model, demonstrating potent agonistic activity (EC50: 17 nM). This compound is applicable in researching monogenic autoinflammatory diseases such as SAVI.

H-151 Alkyne (Compound H-151-AL) is a selective inhibitor of STING (stimulator of interferon genes). It shows promise for research in autoimmune diseases, including systemic lupus erythematosus, scleroderma, and autoinflammatory diseases.

NLRP3 modulator 8 (Compound 14) is an NLRP3 regulator that can significantly degrade the NEK7 protein (DC50 = 9 nM). In macrophages, NLRP3 modulator 8 can inhibit the activity of caspase-1 in a dose-dependent manner and reduce the release of IL-1β triggered by the activation of the NLRP3 inflammasome. NLRP3 modulator 8 is applicable for the research of various diseases, including autoinflammatory and autoimmune diseases, neurodegenerative diseases, as well as cardiovascular and metabolic-related diseases, etc.

RIPK2-IN-2 (example 25) is a RIP2 kinase PROTAC inhibitor that effectively blocks RIP2-dependent pro-inflammatory signaling and regulates RIP2 kinase activity in autoinflammatory diseases [1].

Camoteskimab (AVTX-007), a fully human, high-affinity anti-IL-18 monoclonal antibody, holds promise for research into autoinflammatory diseases, such as adult-onset Still's disease (AOSD) [1].

PROTAC STING Degrader-2 is a protein degrader targeting the Stimulator of interferon genes (STING) with a DC50 of 0.53 μM. It induces STING protein degradation by covalently binding to both the STING protein and an E3 ubiquitin ligase. This compound is useful for studying the role of STING in autoinflammatory and autoimmune diseases.

Astin C (Asterin), a naturally occurring cyclic peptide that can be extracted from Aster tataricus, specifically blocks IRF3 recruitment at the STING signalosome inhibiting cGAS-STING signaling and innate inflammatory responses triggered by cytoplasmic dna, resulting in mice that are more susceptible to HSV-1 infection and significantly attenuating autoinflammatory responses.