Vacuolin-1

Catalog No.S6912 Batch:S691201

Technical Data

Formula

C₂₆H₂₄IN₇O

Molecular Weight

577.42

CAS No.

351986-85-1

Solubility (25°C)*

In vitro

DMSO

10 mg/mL (17.31 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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.

Targets

PIKfyve ^[1]

In vitro

Vacuolin-1 blocks both ionophore- and wound-induced, Ca²⁺-dependent exocytosis of lysosomes, but does not block Ca²⁺-dependent fusion of enlargeosomes with the plasma membrane.^[1]

In vivo

Vacuolin-1 significantly suppresses the metastasis and/or tumor growth of breast cancer or melanoma. Vacuolin-1 targets Capping protein Zβ (CapZβ) to inhibit endosomal trafficking and metastasis.^[3]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Human HeLa cells, Human A431 cells, monkey BSC-1 cells Concentrations 1 μM-10 μM Incubation Time 20-180 min Method HeLa cells grown on 25 mm diameter coverslips in six-well plates are incubated for 10 min with BSA conjugated with 5 nm gold particles, followed by a 3–12 h incubation in a medium without BSA–gold. During the last 20–180 min of the chase, the cells are incubated in 0.2% DMSO with or without 1 μM vacuolin-1. For electron microscopy, cells are washed with PBS, fixed at room temperature for 30 min, and processed for ultrathin cryosectioning and immunolabelling.

Cell Assay:^{^[1]}

Cell lines
Human HeLa cells, Human A431 cells, monkey BSC-1 cells
Concentrations
1 μM-10 μM
Incubation Time
20-180 min
Method
HeLa cells grown on 25 mm diameter coverslips in six-well plates are incubated for 10 min with BSA conjugated with 5 nm gold particles, followed by a 3–12 h incubation in a medium without BSA–gold. During the last 20–180 min of the chase, the cells are incubated in 0.2% DMSO with or without 1 μM vacuolin-1. For electron microscopy, cells are washed with PBS, fixed at room temperature for 30 min, and processed for ultrathin cryosectioning and immunolabelling.

References

Selleck's Vacuolin-1 has been cited by 5 publications

Coxiella burnetii effector CvpE maintains biogenesis of Coxiella-containing vacuoles by suppressing lysosome tubulation through binding PI(3)P and perturbing PIKfyve activity on lysosomes [ Virulence, 2024, 15(1):2350893]	PubMed: 38725096
Coxiella burnetii effector CvpE maintains biogenesis of Coxiella-containing vacuoles by suppressing lysosome tubulation through binding PI(3)P and perturbing PIKfyve activity on lysosomes [ Virulence, 2024, 15(1):2350893]	PubMed: 38725096
Induction of lysosomal exocytosis and biogenesis via TRPML1 activation for the treatment of uranium-induced nephrotoxicity [ Nat Commun, 2023, 14(1):3997]	PubMed: 37414766
Induction of lysosomal exocytosis and biogenesis via TRPML1 activation for the treatment of uranium-induced nephrotoxicity [ Nat Commun, 2023, 14(1):3997]	PubMed: 37414766
Endocytosis, Distribution, and Exocytosis of Polystyrene Nanoparticles in Human Lung Cells [ Nanomaterials (Basel), 2022, 13(1)84]	PubMed: 36615994

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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