tmem173

Omaveloxolone (RTA-408) (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.

Vadimezan (DMXAA) is a vascular disrupting agent, a murine STING agonist, and an inducer of cytokines such as type I IFN. Vadimezan has antitumor activity and induces a rapid cessation of blood flow in tumors without affecting blood flow in normal tissues.

SR-717 is a cGAMP analog, a non-nucleoside STING agonist that induces a closed activation conformation of STING. SR-717 has antitumor activity and promotes activation of immune cells and cross-presentation of antigens.

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]

C-176 (STING inhibitor 1) is a STING inhibitor with selectivity and blood-brain barrier permeability. C-176 inhibits STING-mediated IFNβ production and possesses anti-inflammatory activity.

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.

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

CCCP (Carbonyl Cyanide m-Chlorophenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. CCCP inhibits the activation of STING and its downstream signaling molecules TBK1 and IRF3.

ADU-S100 ammonium salt is an activator of stimulator of interferon genes (STING). ADU-S100 ammonium salt leads to potent and systemic tumor regression and immunity.

SN-011 (GUN35901) is a STING inhibitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING- mediated disease. It is a demethyl analogue of DUN99845.

SN-008 is a less active analog SN-011 which is a STING antagonist. SN-008 can be used as a negative control.

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

ChX710 activates the type I interferon response to cytosolic DNA by priming specific Interferon-Stimulated Genes (ISGs), inducing the ISRE promoter sequence, and facilitating the phosphorylation of Interferon Regulatory Factor (IRF) 3.

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.

STING agonist-4 is an agonist of stimulator of Interferon Genes (STING) receptor(IC50 of 20 nM).

C-178 is a covalent inhibitor of STING, binds to Cys91 on STING to block its palmitoylation and prevents recruitment and phosphorylation of TBK1 in HEK293T cells.

STING activator Compound 53 based on an oxindole core structure demonstrated robust on-target functional activation of STING (human EC50 185 nM) in immortalised and primary cells and a cytokine induction fingerprint consistent with STING activation.

BPK-25 is an active acrylamide compound that enhances the degradation of proteins in the nucleosome remodeling and deacetylation (NuRD) complex through a post-translational mechanism involving covalent protein interaction. Additionally, BPK-25 acts as an inhibitor of TMEM173 activation by the cyclic dinucleotide ligand cGAMP.

STING-IN-3 (C-171) is an inhibitor of stimulator of interferon genes (STING). It binds to STING, inhibits its palmitoylation, and prevents the recruitment and phosphorylation of TBK1.