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].
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.