rig-1

RIG-1 modulator 1 is useful for the treatment of viral infections including influenza virus, HBV, HCV and HIV.

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，

CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP synthase inhibitorsJ. Org. Chem.85(3)1579-1600(2020)

CU-76 is an inhibitor of cyclic GMP-AMP synthase (cGAS; IC50= 0.24 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. CU-76 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP synthase inhibitorsJ. Org. Chem.85(3)1579-1600(2020)

Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) 是双链 RNA 的合成类似物，是一种TLR3和视黄酸诱导型基因 I 受体 (RIG-I 和MDA5) 的激动剂。Polyinosinic-polycytidylic acid potassium 可以用作疫苗佐剂，以增强先天性和适应性免疫反应，并改变肿瘤的微环境，还可以直接触发癌细胞发生凋亡 (Apoptosis)。

Poly(I:C):Kanamycin (1:1) sodium是一种复合物。Poly(I:C)是一种合成的双链RNA类似物和一种TLR3与RIG-I MDA5激动剂，能够增强免疫并促进癌细胞凋亡。Kanamycin是一种对革兰氏阴性和阳性细菌都有效的抗菌药物，能够结合70S核糖体亚基。

Antiviralagent 35 (compound 4d) 作为一种口服抗流感病毒药物，针对流感病毒复制的早期阶段有效。该化合物能够阻断流感病毒引发的ROS积聚、自噬及细胞凋亡，同时在肺部感染的小鼠模型中，抑制RIG-1通路所介导的炎症响应。Antiviralagent 35展现出低细胞毒性（CC50>800 μM，MDCK细胞）且对H1N1（A Weiss 43）展现出显著的抗病毒活性，EC50为2.28 μM。