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Chemical Structure| 351986-85-1 Chemical Structure| 351986-85-1

Structure of Vacuolin-1
CAS No.: 351986-85-1

Chemical Structure| 351986-85-1

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Vacuolin-1 is cell-permeable inhibitor of lysosomal exocytosis and can block the Ca2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. Vacuolin-1 is also PIKfyve inhibitor that inhibits late-stage autophagy by impairing lysosomal maturation.

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Product Details of Vacuolin-1

CAS No. :351986-85-1
Formula : C26H24IN7O
M.W : 577.42
SMILES Code : IC1=CC(/C=N/NC2=NC(N(C3=CC=CC=C3)C4=CC=CC=C4)=NC(N5CCOCC5)=N2)=CC=C1
MDL No. :MFCD00321410
InChI Key :JMEJTSRAQUFNOP-TURZUDJPSA-N
Pubchem ID :9661141

Safety of Vacuolin-1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P264-P270-P301+P312-P330-P501

Related Pathways of Vacuolin-1

PI3K-AKT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 cells 1 μM Inhibited the colony formation ability Oncogene. 2021 Mar;40(10):1775-1791.
Human lung cancer stem cells (LCSCs) 1 μM Inhibited the colony formation ability Oncogene. 2021 Mar;40(10):1775-1791.
CNE-1 cells 1 μM Inhibited the colony formation ability Oncogene. 2021 Mar;40(10):1775-1791.
MDA-MB-231 cells 1 μM 18 hours Significantly inhibited the migration and invasion of cancer cells Oncogene. 2021 Mar;40(10):1775-1791.
4T07 cells 1 μM 18 hours Significantly inhibited the migration and invasion of cancer cells Oncogene. 2021 Mar;40(10):1775-1791.
HeLa cells 1 μM 24 hours Inhibited the recycling and degradation of integrins, affecting the dynamics of focal adhesions Oncogene. 2021 Mar;40(10):1775-1791.
4T1 cells 1 μM 18 hours Significantly inhibited the migration and invasion of cancer cells Oncogene. 2021 Mar;40(10):1775-1791.
MA104 cells 5 μM 1 hour To study the inhibitory effect of Vacuolin-1 on VSV-eGFP-SARS-CoV-2 infection, results showed that Vacuolin-1 effectively inhibited VSV-eGFP-SARS-CoV-2 infection Proc Natl Acad Sci U S A. 2020 Aug 25;117(34):20803-20813.
SVG-A cells 5 μM 1 hour To study the inhibitory effect of Vacuolin-1 on VSV-MeGFP-ZEBOV infection, results showed that Vacuolin-1 effectively inhibited VSV-MeGFP-ZEBOV infection Proc Natl Acad Sci U S A. 2020 Aug 25;117(34):20803-20813.
HeLa cells 1 μM 6 hours Inhibited autophagosome-lysosome fusion, leading to accumulation of autophagosomes Autophagy. 2014;10(11):1895-905.
HeLa cells 1 μM Inhibited the fusion of EGFR endosomes with lysosomes 2018;14(1):176-177. doi: 10.1080/15548627.2017.1367474.
Human orthochromatic erythroblasts 5 μM 24 hours To investigate the rescue effect of Vacuolin-1 on U0126-induced enucleation impairment in erythroblasts. Results showed that Vacuolin-1 partially rescued the enucleation blockage caused by U0126 and increased the number and size of vacuoles. Blood Adv. 2021 Nov 23;5(22):4648-4661.
RAW 264.7 cells 1 μM 24 hours To study the inhibitory effect of Vacuolin-1 on exocytosis in macrophages, results showed that Vacuolin-1 could inhibit lysosome-mediated exocytosis Int J Nanomedicine. 2017 Aug 31;12:6383-6398.
NRK cells 5 μM 1 hour To observe the effect of Vacuolin-1 on lysosome morphology, results showed that lysosomes were significantly enlarged after Vacuolin-1 treatment EMBO Rep. 2005 Sep;6(9):843-7.
HeLa cells 1 μM 1 hour To observe the effect of Vacuolin-1 on lysosome morphology, results showed that lysosomes were significantly enlarged after Vacuolin-1 treatment EMBO Rep. 2005 Sep;6(9):843-7.
NB4 cells 0.25 µM 72 hours Vacuolin-1 enhanced RA-induced CD11b expression in NB4 cells. Cell Biosci. 2022 Nov 3;12(1):179.
HL-60 cells 0.25 µM 5 hours, 24 hours, 48 hours, 72 hours Vacuolin-1 enhanced RA-induced differentiation of HL-60 cells, as evidenced by increased CD11b expression, ROS production, and G1/0 cell cycle arrest. Cell Biosci. 2022 Nov 3;12(1):179.
HeLa cells 5 μM or 10 μM 2 hours Inhibits ionomycin-induced release of lysosomal β-hexosaminidase. EMBO Rep. 2004 Sep;5(9):883-8.
BSC-1 cells 1 μM 1 hour Induces vacuole formation in endosomal and lysosomal compartments without affecting markers for Golgi apparatus, ER, and enlargeosomes. EMBO Rep. 2004 Sep;5(9):883-8.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
MMTV-PyMT transgenic mice Mammary adenocarcinoma model Oral 15 mg/kg or 30 mg/kg daily Once daily for 2 months Significantly inhibited tumor growth and metastasis of mammary adenocarcinomas Oncogene. 2021 Mar;40(10):1775-1791.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.66mL

1.73mL

0.87mL

17.32mL

3.46mL

1.73mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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