Vacuolin-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的 PIKfyve 抑制剂，通过损害溶酶体成熟来抑制自噬，通过激活 RAB5A 有效且可逆地抑制自噬体-溶酶体融合。

A potent PIKfyve inhibitor that inhibits autophagy by impairing lysosomal maturation, potently and reversibly inhibits autophagosome-lysosome fusion by activating RAB5A; blocks the Ca(2+)-dependent exocytosis of lysosomes induced by ionomycin or plasma membrane wounding, without affecting the process of resealing, induces the formation of giant vacuoles.

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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Vacuolin 1 | Vacuolin1

Autophagy

Autophagy

Autophagy

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351986-85-1

577.4

C26H24IN7O

>98% (HPLC)

In Vitro:?DMSO : 10 mg/mL (17.32 mM)

IC1=CC(/C=N/NC2=NC(N(C3=CC=CC=C3)C4=CC=CC=C4)=NC(N5CCOCC5)=N2)=CC=C1

(E)-4-(2-(3-iodobenzylidene)hydrazinyl)-6-morpholino-N,N-diphenyl-1,3,5-triazin-2-amine

(-20℃)

With Ice Pack

≥ 2 years