Vacuolin-1
Based on 12 publication(s) in Google Scholar
Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation. Vacuolin-1 can induce vacuole formation and increase the percentage of enucleated cells.
For research use only. We do not sell to patients.
- Purity: 98.54%
- CAS No.: 351986-85-1
- Formula: C26H24IN7O
- Molecular Weight:577.42
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Vacuolin-1
More- Nature. 2025 Oct;646(8086):913-924. [Abstract]
- Nat Commun. 2025 May 27;16(1):4887. [Abstract]
- Adv Sci (Weinh). 2025 Nov 3:e09151. [Abstract]
- Basic Res Cardiol. 2022 Apr 7;117(1):20. [Abstract]
- PLoS Pathog. 2023 Feb 24;19(2):e1011202. [Abstract]
- J Proteome Res. 2024 Oct 4;23(10):4409-4421. [Abstract]
- Exp Cell Res. 2026 Aug 1;461(1):115103. [Abstract]
- Vet Microbiol. 2025 Apr 11:305:110518. [Abstract]
- Mol Cell Biol. 2025;45(3):99-115. [Abstract]
- bioRxiv. 2026 Feb 11.
- bioRxiv. 2024 September 15.
- bioRxiv. 2023 Aug 28.
Customer Validation & Images
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Cell Imaging/Staining
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Cell Migration/Invasion Assay
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | CC50 |
>10 μM
Compound: 62
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Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
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[PMID: 33539089] |
| PC-3 | CC50 |
>10 μM
Compound: 62
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Cytotoxicity against human PC-3 cells
Cytotoxicity against human PC-3 cells
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[PMID: 33539089] |
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[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[1]. 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%)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 351986-85-1
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Appearance Solid
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Molecular Weight 577.42
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Formula C26H24IN7O
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Color White to off-white
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SMILES
IC1=CC(/C=N/NC2=NC(N(C3=CC=CC=C3)C4=CC=CC=C4)=NC(N5CCOCC5)=N2)=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (12)
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Journal Impact Factor
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Most Recent
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Nature
2025 Oct;646(8086):913-924. PMID: 40769205 -
Nat Commun
Clustering of NLRP3 induced by membrane or protein scaffolds promotes inflammasome assembly. [Abstract]2025 May 27;16(1):4887. PMID: 40425567 -
Adv Sci (Weinh)
Depletion of Sorcs3 Activates Totipotency in Mouse Embryonic Stem Cells by Modulating Key Signaling Pathways. [Abstract]2025 Nov 3:e09151. PMID: 41178446 -
Basic Res Cardiol
Blunting TRPML1 channels protects myocardial ischemia/reperfusion injury by restoring impaired cardiomyocyte autophagy. [Abstract]2022 Apr 7;117(1):20. PMID: 35389129 -
PLoS Pathog
2023 Feb 24;19(2):e1011202. PMID: 36827461
Vacuolin-1 purchased from MedChemExpress. Usage Cited in: PLoS Pathog. 2023 Feb 24;19(2):e1011202. [Abstract]
Inhibition of endosomal trafficking reduces HTLV-1 infection. SLB-1 cells were treated with DMSO, 10 μM EGA, 10 μM Vacuolin-1 (Vac-1) or 1 μM apilimod (Api) for 4 h prior to co-culture with CHOK1-Luc cells. The results showed that Vacuolin-1 significantly reduced the infectivity of HTLV-1 in cells. The graph shows luciferase assay results averaged from three replicates for each condition of a single experiment and are representative of three independent experiments; ** p<0.01.
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J Proteome Res
Proteome and Glycoproteome Analyses Reveal Regulation of Protein Glycosylation Site-Specific Occupancy and Lysosomal Hydrolase Maturation by N-Glycan-Dependent ER-Quality Control. [Abstract]2024 Oct 4;23(10):4409-4421. PMID: 39235835 -
Exp Cell Res
2026 Aug 1;461(1):115103. PMID: 42276196 -
Vet Microbiol
Surface expression of PEDV nucleocapsid protein facilitates NK cell-mediated ADCC via anti-N nonneutralizing antibody. [Abstract]2025 Apr 11:305:110518. PMID: 40233683 -
Mol Cell Biol
Kinase Inhibitor-Induced Cell-Type Specific Vacuole Formation in the Absence of Canonical ATG5-Dependent Autophagy Initiation Pathway. [Abstract]2025;45(3):99-115. PMID: 39895059 -
Vacuolin-1 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2026 Feb 11.
Vacuolin-1 (0.1-5 μM; 1-2.5 h). Examples of 3D RI tomograms of vacuolated cells and the corresponding estimated pattern of coexisting morphological phenotypes. Vac:Vacuoline. Acc: Accuracy in the overall sequence prediction. Top sequence: ground truth. Bottom, coloured sequence: estimated profile. Red/green colour in the sequence mark the wrong/correct prediction of a phenotype. Spider graphs summarize for each cell the distribution of its morphological phenotypes and their expression severity.
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Vacuolin-1 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 September 15.
The lysosomal exocytosis inhibitor Vacuolin-1 (0.5-10 μM; 75 min) strongly reduced invasion efficiency of S. aureus JE2 in HeLa cells.
Vacuolin-1 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 September 15.
HeLa cells expressing LAMP1-HiBit were treated with Vacuolin-1 (1 µM; 75 min) in the presence of LgBit and NanoLuc substrate. Lysosomal exocytosis was monitored by measuring chemiluminescence in a Tecan microplate reader.
Vacuolin-1 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 September 15.
HeLa cells expressing LAMP1-HiBit were pretreated with Vacuolin-1 (1 µM; 75 min). Subsequently, cells were infected with S. aureus JE2 (MOI 10), treated with 1 µM ionomycin, or left untreated, and lysosomal exocytosis was determined by measuring chemiluminescence in a Tecan microplate reader 10 min p.i.
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Solvent & Solubility
DMSO : 10 mg/mL (17.32 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1 mg/mL (1.73 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[2]. Osamu Sano, et al. Vacuolin-1 inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition. FEBS Lett. 2016 Jun;590(11):1576-85. [Content Brief]
[3]. Yingying Lu, et al. Vacuolin-1 potently and reversibly inhibits autophagosome-lysosome fusion by activating RAB5A. Autophagy [Content Brief]
[4]. Keerthivasan G, et al. Vesicle trafficking plays a novel role in erythroblast enucleation. Blood. 2010 Oct 28;116(17):3331-40. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7318 mL | 8.6592 mL | 17.3184 mL | 43.2960 mL |
| 5 mM | 0.3464 mL | 1.7318 mL | 3.4637 mL | 8.6592 mL | |
| 10 mM | 0.1732 mL | 0.8659 mL | 1.7318 mL | 4.3296 mL | |
| 15 mM | 0.1155 mL | 0.5773 mL | 1.1546 mL | 2.8864 mL |
Vacuolin-1 Related Classifications
HY-118630 Related Classifications
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