Vacuolin-1

Vacuolin-1 is a potent and cell-permeable inhibitor that blocks the Ca(2+)-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. Vacuolin-1 is also a potent and selective PIKfyve inhibitor, and inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition.

Product information

CAS Number: 351986-85-1

Molecular Weight: 577.42

Formula: C26H24IN7O

Chemical Name: 3-Iodobenzaldehyde [4-(diphenylamino)-6-(4-morpholinyl)-1,3,5-triazin-2-yl]hydrazone

Smiles: IC1=CC(/C=N/NC2N=C(N=C(N=2)N(C2C=CC=CC=2)C2C=CC=CC=2)N2CCOCC2)=CC=C1

InChiKey: JMEJTSRAQUFNOP-TURZUDJPSA-N

InChi: InChI=1S/C26H24IN7O/c27-21-9-7-8-20(18-21)19-28-32-24-29-25(33-14-16-35-17-15-33)31-26(30-24)34(22-10-3-1-4-11-22)23-12-5-2-6-13-23/h1-13,18-19H,14-17H2,(H,29,30,31,32)/b28-19+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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%).

References:

1. Jan Cerny, 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. Osamu Sano, et al. Vacuolin-1 inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition. FEBS Lett. 2016 Jun;590(11):1576-85.
3. Yingying Lu, et al. Vacuolin-1 potently and reversibly inhibits autophagosome-lysosome fusion by activating RAB5A. Autophagy

Products are for research use only. Not for human use.