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编 号:F332481
分子式:C26H24IN7O
分子量:577.42
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5mg
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10mg
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50mg
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100mg
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生物活性:
Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation. Vacuolin-1 can induce vacuole formation and increase the percentage of enucleated cells.

体外研究:
Vacuolin-1 (1 μM; Pretreatment 1 hour) blocks ionomycin-induced exocytosis of lysosomes but not of enlargeosomes. It results in vacuolation of lysosomes (A) and complete inhibition of the surface expression of Lamp-1.?Vacuolin-1 (1 μM; 20-180 min) disrupts the segregation of inner and limiting membranes characteristic of endosomes and lysosomes. Ultrastructural analysis also shows that vacuolin-1 favours fusion of inner and limiting membranes.?Vacuolin-1 (5 or 10 μM; 2 hours) blocks the Ca2+-dependent release of β-hexosaminidase from lysosomes. In HeLa cells, ionomycin results in the expected release of 18-20% of lysosomal β-hexosaminidase. But when cells pretreated with vacuolin-1, releases no more β-hexosaminidase compared with cells that are not exposed to ionomycin (4%).
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