WX8 is a specific inhibitor of PIKfyve, induces accumulation of cytoplasmic vacuoles on osteosarcoma U2OS cells with EC50 of 10 nM.
WX8 induced accumulation of 2 autophagosome biomarkers, the phosphatidylethanolamine conjugate (LC3-II) of MAP1LC3A protein (LC3-I), and the SQSTM1/p62 ubiquitin-binding protein (sequestosome 1)
WX8 inhibited U2OScell proliferation and viability with IC50 of 0.2 and 0.35 uM, respectively.
WX8 impaired lysosomal trafficking, did not impair lysosomal acidity.
WX8 prevented heterotypic fusion of lysosomes with autophagosomes.
Pretreatment of eliminate pluripotent embryonal carcinoma cells (ECCs) with WX8 suppressed their ability to form teratocarcinomas in mice, selectively eliminated pluripotent cells in mice harboring teratocarcinoma xenografts.
