名称 | 4-Octyl itaconate |
描述 | 4-Octyl Itaconate, a cell-permeable derivative of Itaconate, is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1 and inhibits phosphorylation of STING. |
体外活性 | METHODS: Human PBMC cells were pretreated with 4-Octyl Itaconate (62.5-125 μM) for 3 h. The expression levels of target proteins were detected by Western Blot.
RESULTS: 4-Octyl Itaconate decreased LPS-induced pro-IL-1β and HIF-1α protein levels. [1]
METHODS: Macrophage THP1 cells were treated with 4-Octyl Itaconate (200 ng/mL) for 2 h, then stimulated with 2′,3′cGAMP for 1 h. The level of p-STING was detected by Immunofluorescence.
RESULTS: 4-Octyl Itaconate pretreatment resulted in a significant inhibition of STING phosphorylation. [2] |
体内活性 | METHODS: To test the anti-inflammatory activity in vivo, 4-Octyl Itaconate (50 mg/kg in 40% cyclodextrin in PBS) was intraperitoneally injected into mice, and 2 h later LPS (2.5 mg/kg) was intraperitoneally injected.
RESULTS: 4-Octyl Itaconate counteracted the pro-inflammatory response to LPS in vivo. 4-Octyl Itaconate activated Nrf2, prolonged survival, decreased clinical scores and improved thermoregulation, and decreased IL-1β and TNF levels, but not IL-10, in the LPS model of sepsis. [1]
METHODS: To investigate the role in immunosuppressive impairment in sepsis, 4-Octyl Itaconate (25-50 mg/kg) was injected intraperitoneally into a C57bl/6 mouse model of sepsis established by cecum ligation and puncture (CLP).
RESULTS: 4-Octyl Itaconate inhibits the early release of inflammatory and oxidative stress-related factors to reduce tissue and organ damage in septic mice. [3] |
存储条件 | 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 : 12.2 mg/mL (50.35 mM), 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. DMSO : 121.95 mg/mL (503.28 mM)
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关键字 | Keap1-Nrf2 | 4-Octyl itaconate | inhibit | Inhibitor | 4 Octyl itaconate | 4Octyl itaconate | 4-Octyl Itaconate |
相关产品 | TBHQ | L-Cystine dihydrochloride | Mangiferin | Pyridoxine | Resveratrol | Luteolin | Curcumin | Ezetimibe | Oltipraz | Pyridoxine hydrochloride |
相关库 | NF-κB 通路分子库 | 表型筛选靶点鉴定库 | 神经退行性疾病化合物库 | 经典已知活性库 | HIF-1化合物库 | PPI抑制剂库 | 抗衰老化合物库 | 化妆品成分化合物库 | 已知活性化合物库 | 转录因子库 |