| Name | 4-Octyl itaconate |
| Description | 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. |
| In vitro | 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] |
| In vivo | 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] |
| Storage | keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 12.2 mg/mL (50.35 mM), Solution.
DMSO : 237.5 mg/mL (980.15 mM), Sonication is recommended.
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| Keywords | Keap1-Nrf2 | Inhibitor | inhibit | 4-Octyl itaconate | 4-Octyl Itaconate | 4Octyl itaconate | 4 Octyl itaconate |
| Inhibitors Related | TBHQ | L-Cystine dihydrochloride | Mangiferin | Dimethyl fumarate | Methyl 3,4-dihydroxybenzoate | Pyridoxine | Resveratrol | Luteolin | Curcumin | Ezetimibe | Oltipraz | Pyridoxine hydrochloride |
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United States
