interferon a 1

Interferon receptor inducer-1 Used in the treatment of a disorder in which the induction of interferon is involved. is an interferon (IFN) receptor inducer.

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.

IFN alpha-IFNAR-IN-1 hydrochloride is an inhibitor of the interaction between IFN-α and IFNAR, effectively inhibiting MVA-induced IFN-α responses by BM-pDCs with an IC50 of 2-8 μM.

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

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.

MG-T-19, a TIM-3 inhibitor (KD=0.26 μM), significantly inhibited the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9, and increased the production of TNF-α and IFN-γ in PBMCs, which reactivated the tumor-attacking ability of T cells.

ADU-S100 (MIW815) is a cyclic dinucleotide (CDN) class STING agonist that significantly induces the production of IFN-β and pro-inflammatory cytokines TNF-α, IL-6, and MCP-1, induces TBK1 and IRF3 phosphorylation, and exhibits antitumour activity.

GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood

KIN1408 is an antiviral small molecule compound that is an agonist of the RIG-1-like receptor (RLR) pathway and is able to drive the activation of IRF3 (Interferon Regulatory Factor 3) to induce the expression of innate immunity genes (e.g., MDA5, RIG-1, Mx1, IRF7, and IFIT1), and to promote the nuclear translocation of IRF3 by targeting MAVS (Mitochondrial Antiviral Signaling Protein) or its upstream IRF3 nuclear translocation by targeting MAVS (mitochondrial antiviral signaling protein) or its upstream factors. KIN1400 is the parent, and KIN1409 is a derivative.

XYL-1 is a potent PARP7 inhibitor with an IC50 of 0.6 nM. It has the capability to enhance type I interferon signaling in vitro, positioning it as a potential candidate for the development of cancer immunotherapy drugs.

IRF1-IN-2 is a small molecule inhibitor of interferon regulatory factor 1 (IRF1) that functions by reducing the binding affinity of IRF1 for the caspase-1 (CASP1) gene promoter. this inhibition subsequently suppresses critical cell death signaling pathways, such as pyroptosis, and provides robust protection against ionizing radiation-induced skin inflammatory damage in preclinical models.

BTN3A1 ligand-1 (Compound 26b) is an aryl/acylalkyl phosphonate prodrug containing a triazole group. It is capable of stimulating T cell proliferation (EC50: 0.49 nM) and promoting interferon γ secretion. Additionally, this compound exhibits a degree of plasma stability, making it relevant for research in immunotherapy.

hSTING activator-1 (Compound 68) is a STING agonist capable of effectively activating various human STING variants (R232, H232, HAQ), with EC50 values of 56 nM, 89 nM, and 51 nM, respectively. This compound activates the type I interferon pathway by directly binding to the STING protein and stabilizing its conformation, which leads to downstream IRF3 phosphorylation and cytokine release. hSTING activator-1 also demonstrates potential in cancer research by inhibiting fibrosarcoma tumor growth.

KRN7000 analog 1 stimulates a strong Th1-biased immune response by inducing interferon-γ (IFN-γ) and reducing interleukin-4 (IL-4). This compound shows potential as an antitumor agent and vaccine adjuvant.

IRF1 antagonist 1 (8003-3282) is a potent antagonist of IRF1 (interferon regulatory factor), exhibiting anti-inflammatory properties. This compound helps maintain the integrity of the blood-brain barrier and reduces cerebral edema. Additionally, IRF1 antagonist 1 can enhance neurological outcomes in mouse models of acute traumatic brain injury (TBI).

G3-YSD is a G3 terminal Y-shaped short DNA and functions as a cyclic guanosine-adenosine monophosphate synthase (cGAS) agonist. It serves as a minimal immunostimulatory DNA motif, capable of activating the DNA sensor cGAS, which induces type I interferon in a manner dependent on structure and sequence. G3-YSD is applicable for detecting HIV-1 single-stranded DNA.

BRD0476 is a suppressor of pancreatic β-cell apoptosis. BRD0476 inhibits interferon-gamma (IFN-γ)-induced Janus kinase 2 (JAK2) and signal transducer and activation of transcription 1 (STAT1) signaling to promote β-cell survival. BRD0476 inhibits JAK-STAT

5'-pApA is a linearized form of cyclic di-AMP, a bacterial second messenger that activates the host innate immune system through stimulator of interferon genes (STING).1,2,3,4It is a metabolite of cyclic di-AMP formedviahydrolysis by various phosphodiesterases (PDEs).55'-pApA is intended for use as a negative control for cyclic di-AMP signaling. 1.Burdette, D.L., Monroe, K.M., Sotelo-Troha, K., et al.STING is a direct innate immune sensor of cyclic-di-GMPNature478(7370)515-518(2011) 2.Parvatiyar, K., Zhang, Z., Teles, R.M., et al.DDX41 recognizes bacterial secondary messengers cyclic di-GMP and cyclic di-AMP to activate a type I interferon immune responseNat. Immunol.13(12)1155-1161(2012) 3.Woodward, J.J., Iavarone, A.T., and Portnoy, D.A.c-di-AMP secreted by intracellular Listeria monocytogenes activates a host type I interferon responseScience328(5986)1703-1705(2010) 4.Witte, C.E., Whiteley, A.T., Burke, T.P., et al.Cyclic di-AMP is critical for Listeria monocytogenes growth, cell wall homeostasis, and establishment of infectionmBio4(3)e00282-00213(2013) 5.Fahmi, T., Port, G.C., and Cho, K.H.c-di-AMP: An essential molecule in the signaling pathways that regulate the viability and virulence of gram-positive bacteriaGenes (Basel)8(8)197(2017)

CAY10748 is an agonist of stimulator of interferon genes (STING; IC50= 0.3794 μM in a competition binding assay).1It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC50s = 0.287 and >100 μM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β and the levels of chemokine (C-X-C motif) ligand 10 (CXCL10), and IL-6 in peripheral blood mononuclear cells (PBMCs) when used at a concentration of 10 μM. It also reduces tumor growth in a CT26 murine colon cancer model when administered at a dose of 0.15, but not 1.5, mg/kg. 1.Xi, Q., Wang, M., Jia, W., et al.Design, synthesis, and biological evaluation of amidobenzimidazole derivatives as stimulator of interferon genes (STING) receptor agonistsJ. Med. Chem.63(1)260-282(2019)

StA-IFN-1 is an inhibitor of the interferon (IFN) induction pathway with an IC50 value of 4.1 μM in a GFP reporter assay for IFN induction similar to TPCA-1 , which specifically inhibits the IKKβ component of the IFN induction pathway. It does not show inhibitory activity in a GFP reporter assay for IFN signaling in which ruxolitinib , which is specific for the IFN signaling component JAK1, is active. StA-IFN-1 reduces the levels of IFN-β, but not ISG MxA, mRNA, suggesting that it is selective for the IFN induction pathway and not the IFN signaling pathway.

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 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 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).

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).