sting agonist-1

STING agonist-1 (G10)是一种人类特异性 STING 激动剂，可引发针对新兴甲病毒的抗病毒活性。它抑制甲病毒属 VEEV 复制，IC90值为 24.57 μM。

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。。

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。

STINGagonist-17 (compound 4a) 是一种有效的STING 激动剂，其IC50值为 0.062 nM，具有抗癌活性，可用于肿瘤免疫。

STINGagonist-13 是一种STING 激动剂，通过STING 介导的免疫激活进行癌症免疫。STINGagonist-13 可刺激STING 下游信号传导并促进 I 型干扰素免疫反应。STINGagonist-13 能显著降低肿瘤体积并具有免疫记忆衍生的癌症抑制活性。

STINGagonist-18（compound 1a）适用于ADCs的合成，例如与Trastuzumab偶联。

hSTING agonist-1 (compound 17) 是一种有效的 hSTING 激动剂，尽管其口服利用度较低，但在炎症研究中具有重要作用。

STING agonist-10 是一种 STING 小分子环脲类的有效激活剂 (EC50: 2600 nM)。STING 激活是一种具有高度潜力的免疫疗法。

STING agonist-11 是一种 STING 小分子环脲类的有效激活剂 (EC50: 18 nM)。STING 激活是一种具有高度潜力的免疫疗法。

STINGagonist-19 用于 ISAC（immune-stimulating antibody conjugates）分子的合成。

STING agonist-18 diTFA (compound 1a) 是用于合成抗体活性分子偶联物 (ADCs) 的关键成分,例如用于Trastuzumab 偶联物的生产.

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激动剂12L是一种刺激干扰素基因(STING)的激动剂。它与野生型STING结合(IC50 = 1.15 µM)，以及STING的R232、AQ和Q变体(IC50分别为1.06、0.61和1.12 µM)，并在THP-1和RAW 264.7细胞中诱导报告基因表达(EC50分别为0.38和12.94 µM)。STING激动剂12L (5 µM)在THP-1细胞中诱导IFNB1、CXCL10和IL6 mRNA的表达。在体内，STING激动剂12L (10 mg/kg)提高了血浆IFN-β水平，并且在B16/F10小鼠黑色素瘤模型中减少了肿瘤体积和肺转移灶的数量。

MSA-2 是可口服的非核苷酸 STING 激动剂，MSA-2 的非共价体系二聚体与 STING 纳摩尔亲和力结合。它在同基因小鼠肿瘤模型中显示抗肿瘤活性，与抗 PD-1 协同作用，可刺激肿瘤分泌干扰素-β，诱导肿瘤消退，具有持久的抗肿瘤免疫。[3]

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.

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)

MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide[1]. MSA-2 dimer (60 mg kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival[1]. MSA-2 dimer (40 mg kg; s.c.; 25 days) induces complete tumor regression[1].MSA-2 dimer (60 mg kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) level in tumors[1].MSA-2 dimer (60 mg kg; s.c.; 4 hours) concentrations is observed in tumors than in plasma or other nontumor tissues [1].MSA-2 dimer (THP-1 cells) induces phosphorylation of both TBK1 and IR. MSA-2 dimer (10 μM and 33 μM; macrophages) induces IFN-β[1].MSA-2 dimer also exhibits dose-dependent antitumor activity when administered by IT, SC, or PO routes[1]. [1]. Pan BS, et al. An orally available non-nucleotide STING agonist with antitumor activity. Science. 2020;369(6506):eaba6098.

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-7 是一种非核苷酸STING 的激动剂，可选择性结合小鼠而非人类 STING。

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].

c-di-AMP (Cyclic diadenylate) sodium 作为一种STING 激动剂，通过结合STING 激活TBK3-IRF3 信号途径，引发I 型 IFN 和 TNF 产生，兼具细菌第二信使功能，在革兰氏阳性细菌中调控细胞生长、存活及毒力，并影响宿主免疫反应。此外，作为有效的粘膜佐剂，它能刺激体液和细胞反应。

IACS-8803 disodium 是一种高效环状二核苷酸的STING 激动剂，具有强大的全身抗肿瘤作用。