Apilimod (mesylate)

Apilimod is an inhibitor of the class III phosphatidylinositol kinase PIKfyve (IC50 = 14 nM). 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-gamma and LPS or the TLR7 agonist R-837 (imiquimod, Cay-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-gamma and S. aureus Cowan I (SAC) in isolated human PBMCs (IC50 = 10 nM). It prevents infection of Vero E6 cells by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2, EC50 = 23 nM). Apilimod reduces cell viability in a panel of B cell non-Hodgkin lymphoma cell lines with a mean IC50 value of 142 nM. 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 (Cay-36727).. SMILES: O=S(O)(C)=O.CC1=CC(/C=N/NC2=NC(OCCC3=NC=CC=C3)=NC(N4CCOCC4)=C2)=CC=C1. InChi Code: InChI=1S/C23H26N6O2.CH4O3S/c1-18-5-4-6-19(15-18)17-25-28-21-16-22(29-10-13-30-14-11-29)27-23(26-21)31-12-8-20-7-2-3-9-24-20,1-5(2,3)4/h2-7,9,15-17H,8,10-14H2,1H3,(H,26,27,28),1H3,(H,2,3,4)/b25-17+,. InChi Key: UDXQXJNZBYATHE-AREUYOMRSA-N