Description
A novel potent, selective, oral PIKfyve inhibitor that selectively decreases c-Rel binding to gene promoters of IL-12p40 and IL-1beta, regulates cytokine production through PIKfyve-c-Rel pathway (IL-12p40 IC50=2nM); inhibits the production of IL-12p40, IL-6 and IL-1beta but not TNFalpha in activated macrophages or dendritic cells, and expression of IgM-induced MHC class II on B cells; reduces Akt phosphorylation in IFNgamma/LPS-stimulated RAW264.7 cells, greatly increases cell size with many small vesicles in the cytoplasm; prevents the development of arthritis in rats