| Description | H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo. |
| In vitro | 方法：小鼠单核巨噬细胞 RAW264.7 用 H-151 (0.25-2 μM) 处理 1 h，随后用 rmCIRP (1 μg/mL) 刺激 24 h，使用 ELISA 检测 IFN-β 水平。结果：用 H-151 预处理的细胞的培养上清液中 IFN-β 呈剂量依赖性降低。H-151 在体外抑制 eCIRP 诱导的 STING 的激活。[1]方法：人单核细胞 THP-1 用 H-151 (0.5 μM) 处理 2 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：H-151 抑制 TBK1 磷酸化，H-151有效抑制 hsSTING。[2] |
| In vivo | 方法：为检测体内活性，将 H-151 (750 nmol，200 μL) 腹腔注射给 Trex1-/-Ifnb1Δβ-luc/Δβ-luc 报告小鼠，每天一次，持续七天。结果：当给药一周时，H-151 在表达生物发光 IFNβ 报告基因的 Trex1-/- 小鼠中表现出显著的疗效。[2]方法：为检测在顺铂诱导的急性肾损伤 (AKI) 中的作用，将 H-151 (7 mg/kg) 腹腔注射给顺铂诱导 AKI 的 C57BL/6J 小鼠，每天一次，给药三次。结果：H-151 治疗显著改善了顺铂诱导的肾损伤，如肾功能、肾形态和肾脏炎症的改善。H-151 可能是治疗 AKI 的潜在治疗剂，可能通过抑制 STING 介导的炎症和线粒体损伤。[3] |
| molecular weight | 279.34 |
| Molecular formula | C17H17N3O |
| CAS | 941987-60-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 14.08 mg/ml (50.42 mM), Sonication is recommended. DMSO: 55 mg/mL (196.89 mM), Sonication is recommended. |
| References | 1. Kobritz M, et al. H151, A SMALL MOLECULE INHIBITOR OF STING AS A NOVEL THERAPEUTIC IN INTESTINAL ISCHEMIA-REPERFUSION INJURY. Shock. 2022 Sep 1;58(3):241-250. 2. Haag SM, et al. Targeting STING with covalent small-molecule inhibitors. Nature. 2018 Jul;559(7713):269-273. 3. Gong W, et al. The novel STING antagonist H151 ameliorates cisplatin-induced acute kidney injury and mitochondrial dysfunction. Am J Physiol Renal Physiol. 2021 Apr 1;320(4):F608-F616. |
| Citations | 1. Song P, Yang W, Lou K F, et al. UNC13D inhibits STING signaling by attenuating its oligomerization on the endoplasmic reticulum. EMBO reports. 2022: e55099 2. Chen Q, Tang L, Zhang Y, et al. STING up-regulates VEGF expression in oxidative stress-induced senescence of retinal pigment epithelium via NF-κB/HIF-1α pathway. Life Sciences. 2022: 120089. 3. Qiao W, Hu C, Ma J, et al.Low-dose metronomic chemotherapy triggers oxidized mtDNA sensing inside tumor cells to potentiate CD8+ T anti-tumor immunity.Cancer Letters.2023: 216370. 4. Li J, Sun Y, Zhao X, et al.Radiation induces IRAK1 expression to promote radioresistance by suppressing autophagic cell death via decreasing the ubiquitination of PRDX1 in glioma cells.Cell Death & Disease.2023, 14(4): 1-16. 5. Qiao W, Chen J, Zhou H, et al.A Single‐Atom Manganese Nanozyme Mn‐N/C Promotes Anti‐Tumor Immune Response via Eliciting Type I Interferon Signaling.Advanced Science.2024: 2305979. 6. Wang Z, Zhang X, Luo Y, et al.Therapeutic targeting of ARID1A-deficient cancer cells with RITA (Reactivating p53 and inducing tumor apoptosis).Cell Death & Disease.2024, 15(5): 375. |