| 名称 | H-151 |
| 描述 | 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. |
| 体外活性 | METHODS: Mouse monocyte macrophage RAW264.7 was treated with H-151 (0.25-2 μM) for 1 h, and then stimulated with rmCIRP (1 μg/mL) for 24 h. The level of IFN-β was measured by ELISA.
RESULTS: IFN-β was dose-dependently reduced in the culture supernatant of cells pretreated with H-151, which inhibited eCIRP-induced activation of STING in vitro. [1]
METHODS: Human monocytes THP-1 were treated with H-151 (0.5 μM) for 2 h, and the expression levels of target proteins were measured by Western Blot.
RESULTS: H-151 inhibited the phosphorylation of TBK1, and H-151 effectively inhibited the activation of hsSTING. [2] |
| 体内活性 | METHODS: To assay in vivo activity, H-151 (750 nmol, 200 μL) was administered intraperitoneally to Trex1-/- Ifnb1Δβ-luc/Δβ-luc reporter mice once daily for seven days.
RESULTS: When administered for one week, H-151 showed significant efficacy in Trex1-/- mice expressing a bioluminescent IFNβ reporter gene. [2]
METHODS: To test the role in cisplatin-induced acute kidney injury (AKI), H-151 (7 mg/kg) was administered intraperitoneally to C57BL/6J mice with cisplatin-induced AKI three times a day.
RESULTS: H-151 treatment significantly ameliorated cisplatin-induced renal injury, as evidenced by improvement in renal function, renal morphology, and renal inflammation.H-151 may be a potential therapeutic agent for the treatment of AKI, possibly by inhibiting STING-mediated inflammation and mitochondrial damage. [3] |
| 存储条件 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 12.5 mg/mL (44.75 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
Ethanol : 14.08 mg/ml (50.42 mM), Sonication is recommended.
DMSO : 55 mg/mL (196.89 mM), Sonication is recommended.
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| 关键字 | ERIS | phosphorylation | Stimulator of Interferon Genes | palmitoylatio | TMEM173 | MPYS | H 151 | inhibit | autoinflammatory | H-151 | TBK1 | STING | H151 | Inhibitor | MITA |
| 相关产品 | SR-717 | ChX710 | SN-008 | Vadimezan | Dazostinag disodium | C-176 | Cridanimod | CCCP | diABZI STING agonist-1 trihydrochloride | MSA-2 | STING activator Compound 53 | C-178 |
| 相关库 | 非甾体类抗炎化合物库 | 经典已知活性库 | 抑制剂库 | NO PAINS 化合物库 | 肿瘤免疫治疗小分子化合物库 | 已知活性化合物库 | 共价抑制剂库 |
United States
