3133-16-2

4-Octyl Itaconate increases nuclear factor erythroid 2-related factor 2 (Nrf2) protein levels and expression of Nrf2 target genes and enhances LPS-induced Nrf2 stabilization in mouse macrophages. In vivo, 4-octyl itaconate (50 mg/kg) decreases serum levels of IL-1β and TNF-α, increases Nrf2 protein expression, and protects against LPS-induced lethality in wild-type, but not Nrf2 knockout, mice.

4-Octyl itaconate (4-OI) possesses anti-inflammatory effects. It can obstruct glyceraldehyde 3-phosphate dehydrogenase (GAPDH) and glycolysis in macrophages. It can be a good substitute to itaconate due to its thiol reactivity. The electrophilic α and β-unsaturated moieties of 4-OI might help to alkylate the thiol in cysteine residues of proteins through Michael reaction.''The endogenous metabolite itaconate has recently emerged as a regulator of macrophage function. 4-Octyl itaconate is a cell-permeable itaconate derivative th at decreases cytokine production and is protective against lipopolysaccharide-induced lethality in vivo. Esterases in mouse myoblast cells and macrophages hydrolyze it to itaconatewhich alkylates cysteine residues on KEAP1allowing the transcription factor Nrf2 to increase the expression of anti-oxidant and anti-inflammatory downstream genes.

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