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Vacuolin-1 PIKfyve inhibitor

Name: Vacuolin-1
Brand: Selleck Chemicals
SKU: S6912
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S6912

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. This compound is also a potent and selective PIKfyve inhibitor, and inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition.

Chemical Structure

Molecular Weight: 577.42

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S691201 DMSO]10 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.86%

99.86

Related Targets	PI3K Akt mTOR AMPK GSK-3 ATM/ATR DNA-PK PDPK1 PTEN PP2A PDK PI4K MELK
Related Products	YM201636 Apilimod MOMIPP

Chemical Information, Storage & Stability

Molecular Weight	577.42	Formula	C₂₆H₂₄IN₇O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	351986-85-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	IC1=CC=CC(=C1)/C=N/NC2=NC(=NC(=N2)N(C3=CC=CC=C3)C4=CC=CC=C4)N5CCOCC5

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (17.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.87mM)	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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.87mM)	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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. This compound targets Capping protein Zβ (CapZβ) to inhibit endosomal trafficking and metastasis.^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/15332114/ [2] https://pubmed.ncbi.nlm.nih.gov/27135648/ [3] https://pubmed.ncbi.nlm.nih.gov/33564074/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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