Vacuolin-1 |
| رقم الكتالوجGC10325 |
Vacuolin-1 هو مثبط إفراز الخلايا الليزوزومية قوي ونفاذ للخلايايحجب Vacuolin-1 خروج الخلايا المعتمد على Ca2 +- ويمنع إطلاق المحتوى الليزوزومي دون التأثير على عملية إعادة الختمVacuolin ‐ 1 هو مثبط قوي وانتقائي PIKfyve ويثبط الالتهام الذاتي في المرحلة المتأخرة عن طريق إضعاف النضج الليزوزومي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 351986-85-1
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Vacuolin-1 is an effective PIKfyve inhibitor that can protect lysosome maturation to inhibit autophagy[1]. Vacuolin-1 can also specifically regulate intracellular vesicle transport and lysosome function by inhibiting cell permeation and lysosome exocytosis[2]. Vacuolin-1 can be used to prevent viral infections, including Ebola virus and SARS-CoV-2[3]. Vacuolin-1 can protect nerve cells by reducing α-synuclein aggregation[4].
In vitro, after pre-treatment of HL-60 myeloid leukemia cells with Vacuolin-1 (0.25μM), followed by co-treatment with all-trans retinoic acid (1μM) for 24–72h, Vacuolin-1 significantly enhanced the expression of the cell differentiation marker CD11b, the production of reactive oxygen species (ROS), and G1/0 phase cell cycle arrest[5]. After pre-treatment of RBL-2H3 cells and mouse bone marrow-derived mast cells (BMMCs) with Vacuolin-1 (10μM) for 3h, Vacuolin-1 can induce the formation of a large number of vacuoles in both cell types. Vacuolin-1 significantly enhanced exocytosis and membrane repair capacity in RBL-2H3 cells, but inhibited these functions in BMMCs[6].
In vivo, Vacuolin-1 (15 or 30mg/kg) was administered orally once daily for 2 months to 1-month-old MMTV-PyMT transgenic mice. Vacuolin-1 significantly reduced the number of lung metastases, the weight of breast tumors, and the incidence of breast tumors in mice[7]. Vacuolin-1 (100mg/kg) was administered intraperitoneally once daily for 14 days to 1-month-old HA-DAT knock-in mice. Vacuolin-1 significantly blocked the Amphetamine (Amph)-induced loss of the dopamine transporter (DAT) in the striatum[8].
References:
[1] Sano O, Kazetani K, Funata M, et al. Vacuolin-1 inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition. FEBS Lett. 2016 Jun;590(11):1576-85.
[2] Pronk SD, Schooten E, Heinen J, et al. Single Domain Antibodies as Carriers for Intracellular Drug Delivery: A Proof of Principle Study. Biomolecules. 2021 Jun 22;11(7):927.
[3] Kang YL, Chou YY, Rothlauf PW, et al. Inhibition of PIKfyve kinase prevents infection by Zaire ebolavirus and SARS-CoV-2. Proc Natl Acad Sci U S A. 2020 Aug 25;117(34):20803-20813.
[4] Sanyal A, Scanavachi G, Somerville E, et al. Neuronal constitutive endolysosomal perforations enable α-synuclein aggregation by internalized PFFs. J Cell Biol. 2025 Feb 3;224(2):e202401136.
[5] Zhu K, Kazim N, Yue J, et al. Vacuolin-1 enhances RA-induced differentiation of human myeloblastic leukemia cells: evidence for involvement of a CD11b/FAK/LYN/SLP-76 axis subject to endosomal regulation that drives late differentiation steps. Cell Biosci. 2022 Nov 3;12(1):179.
[6] Shaik GM, Dráberová L, Heneberg P, et al. Vacuolin-1-modulated exocytosis and cell resealing in mast cells. Cell Signal. 2009 Aug;21(8):1337-45.
[7] Ye Z, Wang D, Lu Y, et al. Vacuolin-1 inhibits endosomal trafficking and metastasis via CapZβ. Oncogene. 2021 Mar;40(10):1775-1791.
[8] Bagalkot T, Sorkin A. Amphetamine Induces Sex-Dependent Loss of the Striatal Dopamine Transporter in Sensitized Mice. eNeuro. 2024 Jan 29;11(1):ENEURO.0491-23.2023.
| Cell experiment [1]: | |
Cell lines | RBL-2H3 cells (rat basophilic leukemia cell line) and BMMCs (mouse bone marrow-derived mast cells). |
Preparation Method | RBL-2H3 cells were maintained in complete culture medium (CCM) consisting of Eagle's minimum essential medium with Earle's balanced salt solution, supplemented with 10% heat-inactivated fetal calf serum (FCS), 4mM L-glutamine, and antibiotics at 37°C in a humidified atmosphere with 5% CO₂. BMMCs were cultured in complete Iscove's medium (CIM) supplemented with antibiotics, 10% FCS, SCF (40ng/ml), and IL-3 (20ng/ml) at 37°C in 10% CO₂. Cells were treated with Vacuolin-1 (10μM) for 3 hours. |
Reaction Conditions | 10μM; 3h |
Applications | Vacuolin-1 can induce the formation of a large number of vacuoles in two types of cells. Vacuolin-1 significantly enhances exocytosis and membrane repair capacity in RBL-2H3 cells but inhibits these functions in BMMCs. |
| Animal experiment [2]: | |
Animal models | Male HA-DAT knock-in mice |
Preparation Method | Mice were intraperitoneally administered with Vacuolin-1 (2mg/kg) 2 hours before saline or amphetamine challenge on Day 14 of the sensitization protocol. Striatal synaptosomes were prepared 1 hour after saline/amphetamine challenge injections for analysis. |
Dosage form | 2mg/kg; i.p. |
Applications | Vacuolin-1 blocked the amphetamine-induced decrease in the HA-DAT protein in the striatal synaptosomes of sensitized male mice. |
References: | |
| Cas No. | 351986-85-1 | SDF | |
| Chemical Name | 3-iodo-2-[4-(diphenylamino)-6-(4-morpholinyl)-1,3,5-triazin-2-yl]hydrazone, benzaldehyde | ||
| Canonical SMILES | IC1=CC(/C=N/NC2=NC(N(C3=CC=CC=C3)C4=CC=CC=C4)=NC(N5CCOCC5)=N2)=CC=C1 | ||
| Formula | C26H24IN7O | M.Wt | 577.4 |
| الذوبان | ≤5mg/ml in DMSO;3mg/ml in dimethyl formamide | Storage | Store at -20°C, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7319 mL | 8.6595 mL | 17.319 mL |
| 5 mM | 346.4 μL | 1.7319 mL | 3.4638 mL |
| 10 mM | 173.2 μL | 866 μL | 1.7319 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.)
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *