Apilimod

PIKfyve抑制剂(IC50=14nM)；对PIKfyve具有选择性，优于其他10种脂质激酶和31种蛋白激酶（所有IC50s=>9.1µM）；抑制IFN-γ和LPS或R-837在分离的人PBMCs中诱导的IL-12p40的产生（IC50s分别为2.4和3nM）以及IFN-γ和SAC在分离的人PBMCs中诱导的IL-23的产生（IC50=10nM）；预防SARS-CoV-2感染VeroE6细胞（EC50=23nM）；降低一组B细胞非霍奇金淋巴瘤细胞系的细胞活力（平均IC50=142nM）；10mg/kg剂量可降低CD4+CD45RbhighT细胞移植小鼠IBD模型中的疾病严重程度；降低IRBP1-20诱发的实验性自身免疫性葡萄膜视网膜炎小鼠模型中的疾病严重程度。An inhibitor of PIKfyve (IC50 = 14 nM); is selective for PIKfyve over 10 other lipid kinases and 31 other protein kinases (IC50s = >9.1 µM for all); inhibits the production of IL-12p40 induced by IFN-γ and LPS or R-837 in isolated human PBMCs (IC50s = 2.4 and 3 nM, respectively) and the production of IL-23 induced by IFN-γ and SAC in isolated human PBMCs (IC50 = 10 nM); prevents infection of Vero E6 cells by SARS-CoV-2 (EC50 = 23 nM); reduces cell viability in a panel of B cell non-Hodgkin lymphoma cell lines (mean IC50 = 142 nM); decreases disease severity in a CD4+CD45Rbhigh T cell transfer mouse model of IBD at 10 mg/kg; decreases disease severity in a mouse model of IRBP1-20-induced experimental autoimmune uveoretinitis.