351986-85-1|4-(2-(3-Iodobenzylidene)hydrazinyl)-6-morpholino-N,N-diphenyl-1,3,5-triazin-2-amine|CsnPharm

CAS No.: 351986-85-1

Vacuolin-1 Catalog No. CSN27620

Vacuolin-1 is cell-permeable inhibitor of lysosomal exocytosis and can block the Ca2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. Vacuolin-1 is also PIKfyve inhibitor that inhibits late-stage autophagy by impairing lysosomal maturation.

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实验方案

技术信息

生物活性

描述Exocytic fusion of lysosomes triggered by plasma membrane damage is proposed to be the major source of the membrane required for resealing. Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor which blocks the Ca²⁺-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing^[1]. Vacuolin-1 is also a potent inhibitor of the phosphatidylinositol phosphate kinase, PIKfyve with a K_d of 32 nM. In H4 cells expressing mCherry-GFP LC3, vacuolin-1 (3 μM; 24 hr) induced the accumulation of AcGFP- and mCherry-positive puncta, indicating that vacuolin-1 inhibits autophagy by inhibiting the degradation step of autophagosome. In HeLa cells, vacuolin-1 (3 μM; 24 hr) decreased mature cathepsin D levels and increased immature cathepsin D levels, suggesting that vacuolin-1 impairs the endosomal trafficking of de novo synthesized lysosomal enzymes, which in turn results in the suppression of the lysosomal degradation pathway. Moreover, vacuolin-1 treatment induced enlarged M6PR-positive vesicle formation (M6PR is a marker of transport between Golgi bodies and lysosomes) in HeLa cells, further suggesting that vacuolin-1 inhibits autophagy by inhibiting the maturation of lysosomes^[2].
参考文献

[1] Cerny J, et al. The small chemical vacuolin-1 inhibits Ca(2+)-dependent lysosomal exocytosis but not cell resealing. EMBO Rep. 2004 Sep;5(9):883-8
[2] Sano O, et al. Vacuolin-1 inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition. FEBS Lett. 2016 Jun;590(11):1576-85

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7318 mL
- 8.6592 mL
- 17.3184 mL
- 5 mM
- 0.3464 mL
- 1.7318 mL
- 3.4637 mL
- 10 mM
- 0.1732 mL
- 0.8659 mL
- 1.7318 mL

技术信息

CAS号

351986-85-1

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H24IN7O

运输

蓝冰

分子量

577.42

别名

溶解度

DMSO	40.0 mg/mL (69.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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