haq sting

STING ligand-1 是一种 STING 通路激动剂，对 HAQ STING 的 IC₅₀ 为 68 nM，在炎症与免疫学研究中具备应用潜力。

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]

hSTING activator-1 (Compound 68) 是一种有效的STING激动剂。它能够激活多种人类STING变体 (R232、H232、HAQ)，其EC50值分别为56 nM、89 nM和51 nM。hSTING activator-1 通过直接结合STING蛋白并稳定其构象来激活I型干扰素信号通路，从而促进IRF3的磷酸化和细胞因子的释放。在抑制纤维肉瘤肿瘤生长方面，hSTING activator-1 显示出在癌症研究中的潜力。

M04 acts as a stimulator of interferon genes (STING) agonist, effectively inducing IFN reporter gene expression in HEK293T cells equipped with wild-type human STING. Its activity is specific, not affecting HEK293T cells with the R71H-G230A-R293Q (HAQ) human STING variant or mouse RAW 264.7 cells, showcasing allelic- and species-dependent effects at a concentration of 75 µM. This compound also stimulates the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At 50 µM, M04 enhances human monocyte-derived dendritic cells' expression of HLA-DR (MHC class II receptor) and co-stimulatory molecules CD40, CD80, and CD86, improving T cell cross-priming in an ex vivo assay.