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Endosomal acidification and autophagy inhibitor
Bafilomycin A1 (BafA1), a macrolide antibiotic isolated from the Streptomyces species, is a specific vacuolar H+ ATPase (V-ATPase) inhibitor. BafA1 prevents the maturation of autophagic vacuoles by inhibiting late-stage fusion between autophagosomes and lysosomes as well as lysosomal degradation . Therefore, it is frequently used to study functional autophagy.
V-ATPases establish and maintain a low luminal pH in endocytic and exocytic compartments. Upon binding to the V-ATPase complex BafA1 inhibits H+ translocation, thereby depriving acidic intracellular compartments (i.e. endosomes, lysosomes, and vesicles) of H+ ions, increasing their pH and inhibiting the function of resident hydrolases. On the other hand, this causes an accumulation of H+ in the cytoplasm of treated cells, leading to acidosis and thus, can cause secondary adverse effects in normal cells .
There is now accumulating evidence demonstrating that BafA1, suppresses the growth of a variety of cancer cells by inhibiting autophagy and inducing apoptotic cell death via various mechanisms [2,3]. An acidic pH is an important feature of the tumor microenvironment and a major determinant of tumor progression, and it is well-established that cancer cells upregulate autophagy as a survival mechanism. Therefore, inhibition of autophagy by BafA1, in combination with anti-cancer therapies (e.g. chemotherapy), represents a promising therapeutic approach that is currently being tested in clinical trials .
Bafilomycin A1 provided by InvivoGen is for research use only.
Key features of Bafilomycin A1:
- Specific and potent V-ATPase inhibitor frequently used to study autophagy
- Inhibitory function validated in cellular assays
- Highly pure (> 90%) and absence of any bacterial contamination has been confirmed
COVID-19 related research
Coronaviruses, such as SARS-CoV and presumably SARS-CoV-2, enter and traffic through the host cell in endosomes. Targeting autophagosome-lysosome fusion and intracellular trafficking with Bafilomycin A1 is one of the strategies to limit SARS-CoV-2 infection.
1. Yamamoto, A. et al. 1998. Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells. Cell Struct Funct 23, 33-42.
2. Yan, Y. et al. 2016. Bafilomycin A1 induces caspase-independent cell death in hepatocellular carcinoma cells via targeting of autophagy and MAPK pathways. Sci Rep 6, 37052.
3. Yuan, N. et al. 2015. Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia. Haematologica 100, 345-356.
Working Concentration: 0.1 - 1 μM
CAS number: 88899-55-2
Solubility: 0.1 mg/ml in DMSO or ethanol
Molecular weight: 622.83 g/mol
- Purity: ≥90% (HPLC)
- The inhibitory activity has been validated using cellular assays.
- The absence of bacterial contamination (e.g. lipoproteins and endotoxins) has been confirmed using HEK-Blue™ hTLR2 and HEK-Blue™ hTLR4 cells.
Bafilomycin A1 is provided as a solid.
- 10 µg Bafilomycin A1
Bafilomycin A1 shipped at room temperature.
Store at -20 ̊C.
Solid product is stable 1 year at -20°C.Back to the top
Chemical structure Bafilomycin A1
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