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-2 is a potent inhibitor of the PIKfyve kinase, with potential applications in cancer and autoimmune disorder research [1].

antibody against human PIKfyve

Apilimod mesylate (STA 5326 mesylate) is a potent IL-12/IL-23 inhibitor.

YM201636 (IC50=33 nM), a specific PIKfyve inhibitor, is less effective to p110α and insensitive to Fabl, which is yeast orthologue.

Apilimod dimesylate is a potent and selective PIKfyve inhibitor. It exhibits no significant activity at other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K. Apilimod dimesylate inhibits cellular entry by SARS-CoV-2, MERS-CoV and MHV S pseudovirions. It reduces the number of SARS-CoV-2-infected hiPSC-derived pneumocyte-like cells by 85% and inhibits SARS-CoV-2 replication in donor lung tissue. It also exhibits selective cytotoxicity in B-cell non-Hodgkin lymphoma compared with normal cells and inhibits production of IL-12 and IL-23. Apilimod dimesylate is also anti-inflammatory and water-soluble.

Apilimod (STA 5326) inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis.

PIK5-12d, a potent PROTAC PIKfyve degrader (DC50: 1.48 nM), effectively induces cytoplasmic vacuolization and inhibits autophagic flux in various prostate cancer cell lines, concurrently halting their proliferation. This compound has demonstrated significant anti-tumor activity [1].

Vacuolin-1 is a cell-permeable inhibitor of Ca2+ dependent fusion of lysosomes to the cell membrane. It acts by inhibiting release of lysosomal content.vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation

APY0201 is a effective, highly specific, ATP-competitive PIKfyve inhibitor (IC50: 5.2 nM). It can interrupt the conversion of phosphatidylinositol 3-phosphate (PtdIns3P) to PtdIns(3, 5)P2.

MOMIPP is a PIKfyve inhibitor and a macropinocytosis inducer. MOMIPP readily penetrates the blood-brain barrier and is moderately effective in suppressing progression of intracerebral glioblastoma xenografts[1][2].