sting agonist-1

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

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.

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

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.

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.

5-HT7 agonist 1 (4-[4-[(2-chlorophenyl)methyl]piperazin-1-yl]-1H-indole) is a selective agonist of 5-HT7 (IC50 = 222.93 nM). 5-HT7 agonist 1 can be used in studies about CNS disorders.

Protease-Activated Receptor-1, PAR-1 Agonist acetate is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist acetate corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].

GLP-1 receptor agonist 9 citrate is an agonist of GLP-1.

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).

CB1 inverse agonist 1 (MRL-650) is an orally active and selective CB1 agonist. The IC50s for CB1 and CB2 are 7.5 nM and 4100 nM, respectively. CB1 inverse agonist 1 shows anorexigenic effects.

D4R agonist-1 is a selective and potent D4R partial agonist (Ki:2.2 nM).D4R agonist-1 can be used to study neurological diseases.

Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM[1].

TREM2 agonist-1 (I-246) is a triggering receptor expressed on myeloid cells-2 (TREM2) agonist (EC50: 3.0 μM-100 μM).This compound is unstable in powder form and other related salt forms are recommended.

A2AR-agonist-1 (N-(2-(1H-Indol-3-yl)ethyl)adenosine) is a potent A2AR and ENT1 agonist (Ki: 4.39 and 3.47 for A2AR and ENT1. It targets the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection.

GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 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 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].

Y4R Agonist-1 is a potent agonist of the Y4 receptor, exhibiting a K_i (inhibition constant) value of 0.048 nM.

TLR4 agonist-1 (TEA, compound 17a) is a potent activator of Toll-like Receptor 4 (TLR4) and prompts the production of MIP-1β in RAW 264.7 and MM6 cells [1].

TLR4 agonist-1 (compound 17a) serves as a potent activator of Toll-like Receptor 4 (TLR4) and stimulates the production of MIP-1β in RAW 264.7 and MM6 cells [1].

Compound 1, identified as a GPR61 inverse agonist, exhibits an IC50 of 11 nM, rendering it suitable for metabolism and body weight disorder research, including obesity and cachexia [1].

Compound 24, a 5-HT2 agonist-1, selectively activates 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50 values of 10 nM, 8.3 nM, and 1.6 nM, respectively. The free base form of this compound is utilized in research pertaining to depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headaches, PTSD, seizure disorders, and additional CNS disorders [1].

TAS2R14 agonist is a potent partial agonist of TAS2R14, displaying an EC50 value of 116.6 ± 23.6 nM [1].

RXFP1 receptor agonist-1 (Example 2), an agonist of the RXFP1 receptor, suppresses cAMP production in HEK293 cells that constitutively express the human RXFP1, exhibiting an EC50 of 300 nM [1].

NLRP3 agonist 1 (compound 23) serves as a potent, orally active agent that activates Caspase-1 enzyme, leading to the cleavage of proinflammatory cytokines pro-IL-1β and pro-IL-18 into their active forms [1].

RORγ inverse agonist 1 has anti-inflammatory activity and can be used to treat rheumatism and psoriasis.

BMP Agonist 1 (compound 2 b) is a small-molecule stimulator of bone morphogenic protein (BMP) signaling, crucial for the differentiation of C2C12 cells. It acts by inhibiting GSK3β and enhancing β-catenin signaling, thereby synergistically modulating Id2 and Id3 expression. This compound is employed in skeletal disease and defect research [1].

Glucocorticoid Receptor Agonist-1 Phosphate Gly-Glu (TFA) serves as a cleavable linker for the synthesis of Antibody-Drug Conjugates (ADCs).

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

GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist , has an EC50 of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes.

Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2 (EC50s: 14.23 μM and 3.34 μM) and is used as a potential treatment for motor nerve terminal dysfunction.

MFN2 agonist-1 (B-A/l) effectively induces mitochondrial fusion in cells deficient in mitofusin 2 (MFN2). It counteracts mitochondrial clumping (formation of static mitochondrial aggregates) and reinstates mitochondrial movement in cultured mouse neurons harboring the CMT2A-associated MFN2 T105M mutation.

HCAR2 agonist 1 (Compound 9n), a G i protein-biased allosteric modulator of HCAR2, activates the G i protein signaling pathway and exhibits anti-inflammatory properties by reducing mRNA levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, and MCP-1). Additionally, it potentiates the anti-inflammatory effects of orthosteric agonists in a mouse model of colitis [1].

β2AR/M-receptor agonist-1 (example 131), a muscarinic antagonist and β2 adrenoceptor agonist (MABA), exhibits dual potency towards β2 adrenoceptor and muscarinic receptor. It demonstrates a significant affinity for the β2 adrenoceptor, indicated by an EC50 value of 9.2 nM, and for the muscarinic receptor with a Ki value of 30.2 nM. Furthermore, its MABA activity is highlighted by an EC50 value of 4.0 nM [1].

RXFP3/4 agonist 1 is a relaxin family peptide 3/4 receptor (RXFP3/4) agonist(EC50s of 82/2 nM, respectivley).

Cisd2 agonist 1 (Compound 4q), with an EC50 of 34 nM, augments Cisd2 expression and ameliorates pathological alterations in fatty liver disease, demonstrating good metabolic stability. This compound is utilized in non-alcoholic fatty liver disease (NAFLD) research[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 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 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].

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

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-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].