sting

diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

STING (WT/R232) activity regulator 126 is a STING modulator with antibacterial and antiviral effects.

STING agonist-30 is a potent STING agonist that triggers STING-dependent immune activation.STING agonist-30 shows broad-spectrum inhibitory effects against a variety of viruses including HSV (Herpes Simplex Virus), rotavirus, and SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus 2).

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

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

STING agonist-23 (CF502) is a non-nucleotide, small-molecule stimulator of the STING pathway. Upon activation, it enhances the phosphorylation of STING, TBK1, and IRF3, leading to elevated levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. Moreover, STING agonist-23 demonstrates efficacy against SARS-CoV series strains [1].

STING agonist-23 (CF505) is a non-nucleotide, small-molecule compound that stimulates STING, enhancing the phosphorylation of STING, TBK1, and IRF3. It elevates the production of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells and demonstrates efficacy against SARS-CoV strains [1].

STING agonist 12L is a stimulator of interferon genes (STING) agonist that exhibits binding affinity for both wild-type STING and its variants R232, AQ, and Q with half-maximal inhibitory concentrations (IC50s) of 1.15 µM for wild-type, 1.06 µM for R232, 0.61 µM for AQ, and 1.12 µM for Q. It effectively induces reporter gene expression in THP-1 and RAW 264.7 cells, with half-maximal effective concentrations (EC50s) of 0.38 µM and 12.94 µM, respectively. At a concentration of 5 µM, STING agonist 12L escalates the expression of IFNB1, CXCL10, and IL6 mRNA in THP-1 cells. When administered in vivo at a dose of 10 mg/kg, it enhances plasma IFN-β levels and considerably reduces tumor volume and the number of lung metastases in a B16/F10 murine melanoma model.

STING agonist-24 (CF504), a non-nucleotide small-molecule STING agonist, activates STING, leading to increased phosphorylation of STING, TBK1, and IRF3. It elevates levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells, demonstrating activity against SARS-CoV series strains [1].

STING-IN-7 (compound 21) serves as a potent inhibitor of the stimulator of interferon genes (STING) pathway, demonstrating an inhibitory concentration (IC50) of 11.5 nM. It effectively hampers the phosphorylation of both STING and interferon regulatory factor 3 (IRF3) [1].

STING agonist-19 serves as a precursor for the synthesis of immune-stimulating antibody conjugates (ISACs).

STING agonist-23 (CF508), a non-nucleotide small-molecule STING agonist, activates STING, thereby enhancing the phosphorylation of STING, TBK1, and IRF3. This activation elevates the production of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. Moreover, STING agonist-23 demonstrates efficacy against SARS-CoV series strains [1].

STING agonist-23 (CF510) is a non-nucleotide, small-molecule activator of the STING pathway. It initiates the phosphorylation of STING, TBK1, and IRF3, enhancing the production of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. Notably, it demonstrates activity against SARS-CoV series strains [1].

STING Agonist-18 (Compound 1a) is a precursor for the synthesis of antibody-drug conjugates (ADCs), including Trastuzumab conjugates [1].

STING agonist 1a is an agonist of stimulator of interferon genes (STING).1It induces expression of an IRF-inducible SEAP reporter gene in a cell-based assay (EC50= 16.77 μM). STING agonist 1a (12.5-100 μM) induces expression of IFN-β, IL-6, and chemokine (C-X-C motif) ligand 10 (CXCL10) in THP-1 cells, an effect that can be reversed by STING knockout or the STING inhibitor H-151 . 1.Hou, H., Yang, R., Liu, X., et al.Discovery of triazoloquinoxaline as novel STING agonists via structure-based virtual screeningBioorg. Chem.100103958(2020)

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

STING-IN-6 (compound 50), a potent inhibitor of STING, exhibits a pIC50 value of 8.9, indicating its significant inhibitory capacity. This compound holds promise for research in immunity [1].

STING agonist-27 (CF509) is a non-nucleotide, small-molecule agonist of STING, which activates STING and demonstrates activity against SARS-CoV series strains [1].

STING agonist 12b is an agonist of stimulator of interferon genes (STING).1It binds to STING (Kd= 26.4 μM) and induces interferon reporter gene expression in cells expressing human or mouse STING (EC50s = 7.45 and 10.23 μM, respectively). STING agonist 12b (40 μM) induces expression of TNF-a, IL-6, IP-10, and IL-1b in THP-1 cells. 1.Hou, S., Lan, X.-j., Li, W., et al.Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonistsBioorg. Chem.95103556(2020)

STING agonist-11 is a potent activator of the small molecule cyclic urea class of STING (EC50: 18 nM).STING activation is a highly promising immunotherapy.

STING ligand-1 is a lead STING ligand(IC50 of 68 nM for HAQ STING).

STING agonist-10 is a potent activator of the STING small molecule cyclic urea class (EC50: 2600 nM).STING activation is a highly promising immunotherapy.

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

STING agonist D61 is a compound that activates the stimulator of interferon genes (STING), leading to the induction of IFN3-inducible secreted alkaline phosphatase (SEAP) and IFN-β-inducible reporter genes in cellular assays, with half-maximal effective concentrations (EC50s) of 52.9 and 116 nM, respectively. At concentrations of 4, 6, and 8 µM, D61 enhances the production of IFN-β and chemokine (C-X-C motif) ligand 10 (CXCL10) mRNA, as well as the phosphorylation of TANK-binding kinase 1 (TBK1), IRF3, and STING in THP-1 monocytes. Additionally, when administered at a dose of 0.25 mg/kg every other day, D61 effectively reduces tumor volume in a CT26 murine colon cancer model without impacting the body weight of the subjects.

STING Agonist-20-Ala-amide-PEG2-C2-NH2 (Compound 30b) TFA, an active compound that interacts with the stimulator of interferon genes (STING), is utilized in the synthesis of immune-stimulating antibody conjugates (ISAC). This compound is also employed in cancer research [1].

PROTAC STING Degrader-1 (Compound SP23) is a STING-targeted PROTAC degrader exhibiting a DC50 of 3.2 μM and demonstrates anti-inflammatory activity [1].

STING Agonist-22 (CF501) is a potent non-nucleotide STING agonist that functions as an adjuvant by activating STING to induce the type I interferon (IFN-I) response and the production of proinflammatory cytokines. It enhances the efficacy of original protein vaccines by providing potent, broad, and long-term immune protection. Additionally, STING Agonist-22 has applications in research on SARS-CoV-2 variants and sarbecovirus diseases [1].

STING agonist-3 trihydrochloride is a selective and non-nucleotide agonist of small-molecule STING(pEC50 and pEC50 of 7.5 and 9.5, respectively), has durable anti-tumor effect and tremendous potential to improve treatment of cancer.

STING agonist-7 is an agonist of non-nucleotide STING that binds selectively to mouse STING but not human STING [1].

diABZI STING agonist-1 is a selective and potent interferon gene-stimulating receptor (STING) agonist with potential antitumor and anti-inflammatory activity for the study of cancer.

STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses grown in THF cells (EC90s = 16.44, 16.7, 18.84, 25.19, and 22.57 μM, respectively), an effect that is dependent on the presence of STING and the IFN-α/β receptor (IFNAR).References1. Gall, B., Pryke, K., Abraham, J., et al. Emerging alphaviruses are sensitive to cellular states induced by a novel small-molecule agonist of the STING pathway. J. Virol. 92(6), e01913-01917 (2018). STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses grown in THF cells (EC90s = 16.44, 16.7, 18.84, 25.19, and 22.57 μM, respectively), an effect that is dependent on the presence of STING and the IFN-α/β receptor (IFNAR). References1. Gall, B., Pryke, K., Abraham, J., et al. Emerging alphaviruses are sensitive to cellular states induced by a novel small-molecule agonist of the STING pathway. J. Virol. 92(6), e01913-01917 (2018).

STING agonist-20, a potent agonist utilized in the synthesis of XMT-2056, serves as a vaccine adjuvant for cancer and various inflammatory immune diseases research.

STING Agonist-13, a stimulator of interferon genes (STING) agonist, enhances cancer immunity through STING-mediated immune activation. It activates STING downstream signaling to promote type I interferon immune responses, significantly reduces tumor volume, and exhibits immunological memory-derived cancer inhibition [1].

STING Agonist-9 (Compound 45) is a powerful stimulator of the STING pathway, demonstrating potent activity with an EC50 of 1.2 nM against human STING (h-STING) and 32.82 μM against mouse STING (m-STING). It exhibits antitumor activity [1].

STING modulator-5 (compound 38), a STING modulator, exhibits a pIC50 value of 9.5 and antagonizes peripheral blood mononuclear cells (PBMC) with a pIC50 value of 8.1. Additionally, it acts as an antagonist of THP-1 cells, making it applicable in immunological disease research [1].

STING agonist-20-Ala-amide-PEG2-C2-NH2, an active scaffolding molecule, engages the stimulator of interferon genes (STING) pathway and can be employed in the synthesis of immune-stimulating antibody conjugates (ISAC). This compound is utilized in cancer research [1].

STING-IN-5, a potent inhibitor of the Stimulator of Interferon Genes (STING) pathway, significantly suppresses lipopolysaccharide (LPS)-induced nitric oxide (NO) synthesis in macrophages, exhibiting an IC50 of 1.15 μM. This compound dampens the inflammatory response and offers potential for research into anti-inflammatory diseases and sepsis [1].

STING agonist-31, a potent STING agonist, exhibits EC50 values of 0.24 μM and 39.51 μM for human STING (h-STING) and murine STING (m-STING), respectively, demonstrating significant antitumor efficacy [1].

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.

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.

STING modulator-3 is a STING inhibitor that effectively inhibits R232 STING, exhibiting a Ki value of 43.1 nM in scintillation proximity assays. Despite its inhibitory action on R232 STING, it does not affect IRF-3 activation or TNF-β induction in THP-1 cells.

STING Modulator-4 is a competitive modulator of STING, exhibiting a K_i value of 0.0933 μM for the R232H STING variant. It demonstrates an EC_50 of over 10 μM for p-IRF3 activation in THP-1 cells.

STING agonist-17 (compound 4a) is a highly potent stimulator of the STING pathway, exhibiting an IC 50 of 0.062 nM. It demonstrates significant anti-cancer properties, promoting tumor immunization [1].

STING Agonist-8 Dihydrochloride (Compound 5-AB) is a highly effective STING agonist, exhibiting an EC50 value of 27 nM in THP1-Dual KI-hSTING-R232 cells.

STING agonist-29 (CF511) is a non-nucleotide small-molecule compound that acts as a STING agonist, effectively activating STING and demonstrating activity against SARS-CoV series strains [1].

STING agonist-3 is a selective and non-nucleotide small-molecule STING agonist(pEC50 and pIC50 of 7.5 and 9.5, respectively), has durable anti-tumor effect and tremendous potential to improve treatment of cancer.

C-176 (STING inhibitor 1) is a strong, covalent mouse STING inhibitor

STING18 is a competitive ligand of stimulator of interferon genes (STING; IC50 = 0.068 μM in a radioligand binding assay).1 It inhibits cGAMP-induced IFN-β production (IC50 = 11 μM) but does not stimulate IFN-β production (EC50 = >30 μM) in THP-1 cells. |1. Siu, T., Altman, M.D., Baltus, G.A., et al. Discovery of a novel cGAMP competitive ligand of the inactive form of STING. Med. Chem. Lett. 10(1), 92-97 (2019).

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.

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