interferon a 1

Interferon receptor inducer-1 是一种干扰素(IFN)受体诱导剂，可用于干扰素诱导参与的紊乱性疾病的研究。

diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) 是一个选择性的干扰素基因刺激受体 (STING) 的激动剂，其在人和小鼠中的 EC50 值分别为 130 nM 和 186 nM。。

IFN alpha-IFNAR-IN-1 hydrochloride 是 IFN-α 和 IFNAR 相互作用的抑制剂。 IFN alpha-IFNAR-IN-1 hydrochloride 抑制 BM-pDCs 的 MVA 诱导的 IFN-α 反应，IC50 为 2-8 μM。

diABZI STING agonist-1 trihydrochloride 是选择性的干扰素基因刺激受体(STING)激动剂，在人和小鼠中都能发挥作用，其 EC50值分别为 130 和 186 nM。

diABZI STING agonist-1 是一种具有选择性和高效性的干扰素基因刺激受体 (STING) 激动剂，具有潜在的抗肿瘤和抗炎活性，可用于研究癌症。

MG-T-19是一种TIM-3抑制剂（KD=0.26 μM），显著抑制TIM-3与PtdSer、CEACAM1和Gal-9的相互作用，增加PBMCs中TNF-α和IFN-γ的产生，从而重新激活T细胞对肿瘤的攻击能力。

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是一种抗病毒的小分子化合物，是RIG-1样 受体 (RLR) 途径的激动剂，能够驱动IRF3（干扰素调节因子 3）激活以诱导先天免疫基因（如 MDA5、RIG-1、Mx1、IRF7 和 IFIT1）表达，也能够通过靶向 MAVS（线粒体抗病毒信号蛋白）或其上游因子，促进 IRF3 的核转位。亲本为KIN1400，同为衍生物的还有KIN1409，

XYL-1，作为一种高效的 PARP7 抑制剂，其 IC50 仅为 0.6 nM。该化合物能够在体外促进Ⅰ型干扰素的信号传导，因此有望作为开发治疗癌症的免疫疗法的潜在药物。

BTN3A1 ligand-1 (Compound 26b) 是一种含三唑的芳基 酰氧基烷基膦酸酯前药，能够刺激 T 细胞增殖 (EC50: 0.49 nM) 并促进干扰素 γ 的分泌。BTN3A1 ligand-1 具有良好的血浆稳定性，适用于相关免疫治疗的研究。

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).

93-O17S is a chalcogen-containing cationic lipidoid.1It has been used in the synthesis of lipid nanoparticles (LPNs) for the delivery of Cre recombinase and ribonucleoproteins for genome editing in mice. LPNs containing 93-O17S have been used for the intratumoral delivery of cGAMP to enhance cross-presentation of tumor antigens and stimulation of interferon genes (STING) activation in a B16 F10 murine melanoma model.2 1.Li, Y., Yang, T., Yu, Y., et al.Combinatorial library of chalcogen-containing lipidoids for intracellular delivery of genome-editing proteinsBiomaterials178652-662(2018) 2.Chen, J., Qiu, M., Ye, Z., et al.In situ cancer vaccination using lipidoid nanoparticlesSci. Adv.7(19)eabf1244(2021)

BSP16 is a highly potent and orally active STING agonist, capable of selectively stimulating the interferon genes pathway. This compound, BSP16, holds great potential for cancer research [1].

PD-L1-IN-1, a powerful PD-L1 inhibitor, demonstrated an IC50 of 115 nM. By forming a robust bond with the PD-L1 protein, PD-L1-IN-1 effectively suppressed tumor growth by enhancing the antitumor immune activity of peripheral blood mononuclear cells in co-cultures with PD-L1 expressing cancer cells (PC9 and HCC827 cells). It significantly elevated the release of interferon γ and induced apoptosis in cancer cells, while exhibiting minimal cytotoxicity in healthy cells [1].

PD-1 PD-L1-IN 6 (compound A13) 是有效的PD-1 PD-L1相互作用抑制剂（IC50为 132.8 nM）。PD-1 PD-L1-IN 6 显示出显著的免疫调节活性。 在 Hep3B OS-8 hPD-L1 与 CD3 T 细胞共培养模型中，PD-1 PD-L1-IN 6显著提高干扰素 -γ 分泌，且无明显毒性作用。 在 T 细胞-肿瘤共培养模型中，PD-1 PD-L1-IN 6恢复免疫应答。

PCC0208018 is a novel activator of effector T cells, enhancing T cell proliferation and activation to release interferon gamma (IFN-γ) and interleukin-2 (IL-2) without blocking the programmed cell death 1 (PD-1) programmed cell death-ligand 1 (PD-L1) binding and not directly affecting tumor cell viability in vitro.

GSK-2245035 maleate is a selective Toll-like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties.