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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-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of Vacuolin-1

PI3K-AKT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
4T1 cells 1 μM 18 hours Significantly inhibited the migration and invasion of cancer cells PMC7946642
HeLa cells 1 μM 6 hours Inhibited autophagosome-lysosome fusion, leading to accumulation of autophagosomes PMC4502727
HeLa cells 1 μM Inhibited the fusion of EGFR endosomes with lysosomes PMC5846563
4T07 cells 1 μM 18 hours Significantly inhibited the migration and invasion of cancer cells PMC7946642
Human lung cancer stem cells (LCSCs) 1 μM Inhibited the colony formation ability PMC7946642
CNE-1 cells 1 μM Inhibited the colony formation ability PMC7946642
A549 cells 1 μM Inhibited the colony formation ability PMC7946642
MDA-MB-231 cells 1 μM 18 hours Significantly inhibited the migration and invasion of cancer cells PMC7946642
HeLa cells 1 μM 24 hours Inhibited the recycling and degradation of integrins, affecting the dynamics of focal adhesions PMC7946642
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 PMC7456157
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 PMC7456157
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. PMC8759143
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 PMC5587219
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 PMC1369166
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 PMC1369166
NB4 cells 0.25 µM 72 hours Vacuolin-1 enhanced RA-induced CD11b expression in NB4 cells. PMC9635152
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. PMC9635152
HeLa cells 5 μM or 10 μM 2 hours Inhibits ionomycin-induced release of lysosomal β-hexosaminidase. PMC1299144
BSC-1 cells 1 μM 1 hour Induces vacuole formation in endosomal and lysosomal compartments without affecting markers for Golgi apparatus, ER, and enlargeosomes. PMC1299144

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 PMC7946642

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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