产品描述:
Apilimod is an inhibitor of the class III phosphatidylinositol kinase PIKfyve (IC50 = 14 nM).{30775} It is selective for PIKfyve over 10 other lipid kinases and 31 other protein kinases (IC50s = >9.1 µM for all). Apilimod inhibits the production of IL-12p40 induced by IFN-γ and LPS or the TLR7 agonist R-837 (imiquimod; Item No. 14956) in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 2.4 and 3 nM, respectively) and the production of IL-23 induced by IFN-γ and S. aureus Cowan I (SAC) in isolated human PBMCs (IC50 = 10 nM).{30775,30778} It prevents infection of Vero E6 cells by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC50 = 23 nM).{67435} Apilimod reduces cell viability in a panel of B cell non-Hodgkin lymphoma cell lines with a mean IC50 value of 142 nM.{67436} It decreases disease severity in a CD4+CD45Rbhigh T cell transfer mouse model of inflammatory bowel disease (IBD) when administered at a dose of 10 mg/kg, as well as in a mouse model of experimental autoimmune uveoretinitis induced by the peptide IRBP1-20 (Item No. 36727).{30778,30776}