sting agonist-3

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.

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-30 是一种高效的 STING 激动剂，能激发STING依赖的免疫激活。STING agonist-30 对包括HSV（单纯疱疹病毒）、轮状病毒及SARS-CoV-2（严重急性呼吸系统综合症冠状病毒2）在内的多种病毒显示出广谱抑制效果。

STINGagonist-31 是一种 STING 激动剂，对 h-STING 和 m-STING 的 EC50值为 0.24 和 39.51 μM。STINGagonist-31 具有抗肿瘤功效。

STINGagonist-33 (example 1) 是一种基于 4-乙基-2-甲基噻唑-5-羧酸的 STING (干扰素基因刺激剂) 激动剂。

STINGagonist-35 (Compound 1a) 是干扰素基因刺激剂 (STING) 的激动剂，激活野生型 STING 和突变型 STING (R232H)，激活率分别为 99% 和 92%。STINGagonist-35 有潜力成为 ADC 药物的有效载荷。

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。。

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]

diABZI-V C-DBCO（Compound 3）作为一种高效的STING激动剂，通过组织蛋白酶B的作用释放diABZI-胺，激活STING，从而使干扰素及其他免疫激活分子的生成得以提高，有效增强免疫系统对肿瘤的攻击能力。在THP1-Dual细胞中，diABZI-V C-DBCO与diABZI-胺激活STING的EC50值分别为1.47 nM和0.144 nM；在原代小鼠脾细胞中，这些值分别为7.7 μM和0.17 μM。因此，diABZI-V C-DBCO在癌症免疫研究领域具有重要的应用价值。

cAIMP作为STING激动剂，在体外的哺乳动物细胞中，与标准的小鼠（DMXAA）和人类（2',3'-cGAMP）STING激动剂相比，cAIMP类似物能更强烈地激活STING依赖的IRF和NF-κB信号通路。在人类血液的离体实验中，它们能诱导I型干扰素（IFNs）和促炎细胞因子的产生。

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)

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).

2',3'-cGAMP-C2-PPA (45) is a cyclic di-nucleotide that acts as a STING agonist (US20210015941A1). It is a drug-linker conjugate for antibody-drug conjugates (ADC) used in the targeted treatment of cancer.

3',3'-cGAMP sodium salt is a STING agonist. Reduces B cell proliferation and induces apoptosis of malignant B cellsin vitro. Suppresses 5TGM1 multiple myeloma xenograft growth in immunodeficient mice, and induces leukemic regression in Eμ-TCL1 mice.

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。

BDW568是一种刺激素干扰素基因（STING）的激动剂，同时是BDW-OH的前药形式。在使用THP-1细胞的报告基因测定中，它能诱导STING转录活性（EC50 = 7.6 µM）。BDW568（50 µM）在THP-1细胞中诱导TANK结合激酶1（TBK1）和IFN调节因子3（IRF3）的磷酸化。