PIKfyve-IN-1 is a cell-active and highly potent chemical probe that can be used for the PIKfyve research in virology. PIKfyve-IN-1 inhibits phosphatidylinositol-3phosphate 5-kinase (PIKfyve) (IC 50 = 6.9 nM)[1].

PIKfyve-IN-1 effectively inhibits the PIKfyve enzyme, as evidenced by its performance in both PIKfyve enzymatic and NanoBRET assays, where it achieves IC 50 values of 6.9 nM and 4.01 nM, respectively [1]. Furthermore, it disrupts coronaviruses' lifecycle by impairing viral replication and entry at concentrations ranging from 0 to 10 μM [1]. Specifically, PIKfyve-IN-1 suppresses MHV and SARS-CoV-2 replication with IC 50 values of 23.5 nM and 19.5 nM, respectively [1]. At a 5 μM concentration, the compound also affects lysosomal homeostasis [1]. In Calu-3 cells, a 1 μM concentration of PIKfyve-IN-1, following a 1-hour incubation, impeded the uptake of a lentivirus pseudotyped with the SARS-CoV-2 spike glycoprotein, as demonstrated through immunofluorescence [1].