Vacuolin-1
PIKfyve inhibitor / Vacuolin-1 (351986-85-1) inhibits autophagy via inhibition of Ca2+-dependent fusion of lysosomes with the plasma membrane and the release of lysosomal content and has no effect on other membrane-bound organelles.1 It has been shown to block endosome maturation by activating RAB5 which compromises the biogenesis and function of lysosomes including autophagosomal-lysosomal fusion and endosomal-lysosomal degradation.2 It potently inhibits migration, invasion and colony formation of cancer cells (which is linked to endosomal trafficking) and targets capping protein Zβ (CapZβ) in these processes.3 Inhibition of lysosomal maturation was shown to be due to potent inhibition of PIKfyve.4
Biochemicals & reagents
351986-85-1
1 Cerny et al. (2004), The small chemical vacuolin-1 inhibits Ca(2+)-dependent exocytosis but not cell resealing; EMBO Rep., 5 883 2 Lu et al. (2014), Vacuolin-1 potently and reversibly inhibits autophagosome-lysosome fusion by activating RAB5A; Autophagy, 10 1895 3 Zuodong et al. (2021), Vacuolin-1 inhibits endosomal trafficking and metastasis via CapZß; Oncogene, 40 1775 4 Sano et al. (2016), Vacuolin-1 inhibits autophagy by impairing lysosomal maturation via PIKfyve; FEBS Lett., 590 1576
-20°C
TARGET: Kinase; Lysosome -- PATHWAY: Autophagy; Cell migration -- RESEARCH AREA: Cell death; Vesicles -- DISEASE AREA: Cancer