IRG1-IN-1

IRG1-IN-1 is an itaconic acid derivative. IRG1-IN-1 can inhibit immune-responsive gene 1 (IRG1) activity. IRG1-IN-1 can be used for the research of cancer, inflammation and autoimmune diseases[1].

Research Areas >> Cancer

Research Areas >> Infection

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

IRG1-IN-1(compound 6) (0.5 mM; 2 mM) reduces production of itaconic acid and the secretion of TNFα from LPS-stimulated human monocyte derived macrophages (hMDMs) [1]. IRG1-IN-1 (0.5 mM; 1 mM) inhibits the proliferation of C-IRG1-9 rat glioma cells[1]. IRG1-IN-1(10 nM) increases proliferation of TCR-activated hCD8+ T cells[1]. IRG1-IN-1(10μM) shows depletion of trimethylation of histone 3 at lysine 4 (H3K4me3) in CR-activated hCD8+ T cells[1]. Western Blot Analysis[1] Cell Line: TCR-activated hCD8+ T cells Concentration: 10 μM Incubation Time: 24-72 h Result: Decreased protein levels of histone 3 (H3). Cell Proliferation Assay[1] Cell Line: C-IRG1-9 rat glioma cells and TCR-activated hCD8+ T cells Concentration: 0.5 mM; 1 mM; 10 nM Incubation Time: 48-96 h Result: Inhibited the proliferation of C-IRG1-9 rat glioma cells and increased proliferation of TCR-activated hCD8+ T cells.

IRG1-IN-1 (compound 6) (i.p.; 0.2 mg/kg; 27 days) shows antitumor effect in C57BL/6 mice[1]. Animal Model: C57BL/6 mice[1] Dosage: 0.2 mg/kg Administration: IP; 27 days Result: Increased survival of C57BL/6 mice bearing mouse CT26 colorectal tumors. Decreased intratumoral frequency of M-MDSCs in tumors.

[1]. Adonia Papathanassiu, et al. Compositions and methods of using itaconic acid derivatives. Patent. US20210261495A1.