Molecular Formula | C26H24IN7O |
Molar Mass | 577.42 |
Density | 1.53±0.1 g/cm3(Predicted) |
Boling Point | 719.7±70.0 °C(Predicted) |
Appearance | White solid |
pKa | 10.74±0.10(Predicted) |
Storage Condition | 2-8°C |
Use | Vacuolin-1 is an effective inhibitor of cell permeation lysosomal exocytosis (lysosomal exocytosis). Vacuolin-1 blocked the lysosomal Ca2 +-dependent exocytosis, preventing the release of lysosomal contents without affecting the re-blocking process. Vacuolin-1 is a potent selective PIKfyve inhibitor that inhibits late autophagy (autophagy) by impairing lysosomal maturation. |
In vitro study | 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. 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. Vacuolin-1 (5 or 10 μM; 2 hours) blocks the Ca 2+ -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%). |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
Reference Show more | 1: Vacuolin-1 potently and reversibly inhibits autophagy by activating Rab5. Autophagy. 2018;14(1):176-177. doi: 10.1080/15548627.2017.1367474. Epub 2018 Feb 1. PubMed PMID: 29388871; PubMed Central PMCID: PMC5846563. 2: Layhadi JA, Fountain SJ. P2X4 Receptor-Dependent Ca(2+) Influx in Model Human Monocytes and Macrophages. Int J Mol Sci. 2017 Oct 27;18(11). pii: E2261. doi: 10.3390/ijms18112261. PubMed PMID: 29077063; PubMed Central PMCID: PMC5713231. 3: Jiang LQ, Wang TY, Webster TJ, Duan HJ, Qiu JY, Zhao ZM, Yin XX, Zheng CL. Intracellular disposition of chitosan nanoparticles in macrophages: intracellular uptake, exocytosis, and intercellular transport. Int J Nanomedicine. 2017 Aug 31;12:6383-6398. doi: 10.2147/IJN.S142060. eCollection 2017. PubMed PMID: 28919742; PubMed Central PMCID: PMC5587219. 4: Li Z, Mbah NE, Maltese WA. Vacuole-inducing compounds that disrupt endolysosomal trafficking stimulate production of exosomes by glioblastoma cells. Mol Cell Biochem. 2018 Feb;439(1-2):1-9. doi: 10.1007/s11010-017-3130-x. Epub 2017 Aug 2. PubMed PMID: 28770472; PubMed Central PMCID: PMC5796851. 5: Chen C, Lu Y, Siu HM, Guan J, Zhu L, Zhang S, Yue J, Zhang L. Identification of Novel Vacuolin-1 Analogues as Autophagy Inhibitors by Virtual Drug Screening and Chemical Synthesis. Molecules. 2017 May 27;22(6). pii: E891. doi: 10.3390/molecules22060891. PubMed PMID: 28555021. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.732 ml | 8.659 ml | 17.318 ml |
5 mM | 0.346 ml | 1.732 ml | 3.464 ml |
10 mM | 0.173 ml | 0.866 ml | 1.732 ml |
5 mM | 0.035 ml | 0.173 ml | 0.346 ml |
biological activity | Vacuolin-1 is a potent cell permeability inhibitor that blocks Ca(2 )-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of re-encapsulation. Vacuolin-1 is also a potent and selective inhibitor of PIKfyve, inhibiting autophagy by inhibiting lysosomal maturation of PIKfyve. |
Target | Value |