Potent (IC50 = 10 nM IFN-g/LPS-stimulated human PMBCs, IC50 = 1 nM in IFN-g/SAC-stimulated human PMBCs) IL-12/IL-23 inhibitor downregulating both at the transcriptional level. Suppresses Th1 but not Th2 immune response.1 Inhibition was also observed in human monocytes, monocyte-derived dendritic cells, and THP-1 cells. Apilimods mechanism of action is mediation of TLR signaling via inhibition of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve, IC50 = 14 nM).2 It displayed selective cytotoxic activity in B-cell non-Hodgkin lymphoma compared with normal cells.3 Apilimod prevented infection of VSV-ZEBOV and VSV-SARS-CoV-2 (IC50 = 50 nM) as well as SARS-CoV-2 strain 2019-nCoVB/USA-1WA/2020.4
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