纯度:99% by HPLC;NMR (Conforms)
分子式:C23H26N6O2
分子量:418.5
溶剂:DMSO (>25 mg/ml)
性状:White solid
存储:-20°C
Activity (short version):IL/12 and 23/PIKfyve inhibitor
Function / Pharmacology:Potent (IC50 = 10 nM IFN-g/LPS-stimulated human PMBC’s; IC50 = 1 nM in IFN-g/SAC-stimulated human PMBC’s) 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. Apilimod’s 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