Apilimod

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).Formal Name: 3-methyl-2-[6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone, benzaldehyde. CAS Number: 541550-19-0. Synonyms: STA-5326. Molecular Formula: C23H26N6O2. Formula Weight: 418.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 20 mg/ml, Ethanol: 10 mg/ml. lambdamax: 231, 262, 322 nm. SMILES: CC1=CC=CC(/C=N/NC2=CC(N3CCOCC3)=NC(OCCC4=NC=CC=C4)=N2)=C1. InChi Code: InChI=1S/C23H26N6O2/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/h2-7,9,15-17H,8,10-14H2,1H3,(H,26,27,28)/b25-17+. InChi Key: HSKAZIJJKRAJAV-KOEQRZSOSA-N.