STING Inhibitor

CCCP is an oxidative phosphorylation (OXPHOS) uncoupler. CCCP induces activation of PINK1 leading to Parkin Ser65 phosphorylation.

C-176 is a selective and blood-brain barrier permeable STING inhibitor. C-176 covalently targets transmembrane cysteine residue 91 and thereby blocking activation-induced palmitoylation of STING.

UM-259 hydrochloride is a STING inhibitor with activity against both murine and human STING (including the STING^R232 mutant). UM-259 hydrochloride inhibits STING-dependent signaling pathways, blocks STING oligomerization, and acts on human primary CD14⁺ monocytes. UM-259 hydrochloride can be used for research on amyotrophic lateral sclerosis, lupus erythematosus, Aicardi-Goutières syndrome, and infant-onset STING-associated vasculopathy.

Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.

SN-011 is a potent and selective mouse and human STING inhibitor, with an IC₅₀ of 76 nM for STING signaling. SN-011 competes with cyclic dinucleotide (CDN) for the binding pocket of the STING dimer, blocking CDN binding and STING activation. SN-011 can be used for the research of STING-driven autoimmune and inflammatory disease.

STING-IN-2 (C-170) is a potent and covalent STING inhibitor. STING-IN-2 efficiently inhibits both mouse STING (mmSTING) and human STING (hsSTING). STING-IN-2 can be used for autoinflammatory disease research.

C-178 is a potent and selective covalent inhibitor of STING. C-178 binds to Cys91 and suppresses the STING responses elicited by distinct bona fide activators in mouse but not human.

Astin C (Asterin) is a cyclopeptide that can be extracted from Aster tataricus. Astin C has anti-inflammatory and anti-cancer activities. Astin C can specifically inhibit the cGAS-STING signaling pathway, block the recruitment of IRF3 to the STING signalosome, and thus inhibit the innate inflammatory response. Astin C can be used in the research of autoimmune diseases and cancers.

LB244 is a homologue of BB-Cl-amidine, which is an orally effective STING inhibitor (EC₅₀=0.8 μM) and can be used to inhibit STING-dependent inflammatory diseases. The pharmacokinetic properties of LB244 indicate limited oral activity in mice.

PROTAC STING Degrader-1 is a PROTAC degrader targeting the STING pathway with a DC₅₀ of 3.2 μM. PROTAC STING Degrader-1 exerts high anti-inflammatory efficacy. PROTAC STING Degrader-1 can be used to study diseases such as acute kidney injury and inflammatory bowel diseases (IBDs).

Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway. Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM_2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes.

STING-IN-3 is an inhibitor of stimulator of interferon genes (STING). STING-IN-3 efficiently inhibits both hsSTING and mmSTING through covalently target the predicted transmembrane cysteine residue 91 and thereby block the activation-induced palmitoylation of STING.

TDI-6570 (TDI-006570) is a blood-brain barrier-permeable, orally active cGAS inhibitor with an IC₅₀ of 1.64 μM. TDI-6570 exhibits high gastrointestinal absorption and a long brain half-life in mice, and shows no toxicity to primary neurons. By inhibiting the cGAS-STING-IFN signaling pathway, TDI-6570 reduces STING levels and the activation of TBK1, blocks double-stranded DNA-induced cGAS activation and downstream interferon-stimulated gene expression, thereby reducing tau protein spread and improving synaptic loss. TDI-6570 reverses memory deficits, increases the amplitude of long-term potentiation, enhances the MEF2C transcriptional network, restores PSD-95 and vGAT punctate structures, and significantly improves cognitive resilience. TDI-6570 can be applied to the research of Alzheimer's disease, Parkinson's disease, systemic lupus erythematosus, as well as various central nervous system and autoimmune diseases.

SN-001 is a STING inhibitor with an IC₅₀ of 3.82 μM.

STING-IN-4 (Compound 1) is a STING inhibitor that inhibits STING expression and hence reducing activation of STING and nuclear factor-κB (NF-κB) signaling. STING-IN-4 shows anti-inflammatory activity and can be used for the research of sepsis.

STING-IN-7 is a potent STING inhibitor with an IC₅₀ of 11.5 nM. STING-IN-7 can inhibit the phosphorylation of STING, IRF3, and TBK1. STING-IN-7 can be used in the research of autoimmune and inflammatory diseases.

JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC₅₀ values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC₅₀ values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD).

Vomicine modulates cGAS-STING-TBK1 signaling pathway, and exhibits anti-inflammatory activity. Vomicine is an alkaloid that can be isolated from Strychnos nux-vomica seeds.

Anti-Mouse myeloperoxidase/MPO Antibody (6G4) is an anti-mouse myeloperoxidase/MPO IgG2c monoclonal antibody. Anti-Mouse myeloperoxidase/MPO Antibody (6G4) can activate the cGAS/STING pathway. Anti-Mouse myeloperoxidase/MPO Antibody (6G4) induces acute and chronic kidney injury in mice. Anti-Mouse myeloperoxidase/MPO Antibody (6G4) is often used in the construction of inflammation conditions models such as anti-neutrophil cytoplasmic antibody (ANCA)-associated vasculitides (AAV).

STING-IN-15 is an orally active STING inhibitor, with an IC₅₀ of 116 nM against h-STING and an IC₅₀ of 96.3 nM against m-STING. STING-IN-15 inhibits the STING signaling pathway in cells, reduces the secretion of IFN-β and IP-10, downregulates the expression of ISG15, ISG56 and TNF-α, and suppresses the phosphorylation of TBK1/IRF3. STING-IN-15 alleviates systemic and renal inflammation induced by STING agonists in mice, reduces tissue damage and the expression of interferon pathway genes, and inhibits spontaneous tissue inflammation in mice. STING-IN-15 can be used for the research of acute kidney injury and autoimmune/inflammatory diseases.