Background
Concanamycin A is a macrolide antibiotic derived from S. diastatochromogenes that is effective against several fungi and yeasts (1). Concanamycin A is an exceptionally potent and specific inhibitor of the ATP-driven proton pumps known as vacuolar type H+-ATPases (V-ATPases). V-ATPases acidify intracellular compartments and translocate protons across the plasma membrane. Intracellular V-ATPases play an important role in endocytosis and intracellular membrane trafficking, while plasma membrane V-ATPases are important in processes such as urinary acidification and bone resorption (2). Treatment of murine cells with Concanamycin A results in apoptosis, evidenced by an increase in fragmented DNA and the number of apoptotic cells with hypodiploid DNA (3). Concanamycin A induced production of nitric oxide and decreased cell growth and survival in mouse leukemic monocyte cells (4). Concanamycin A reversed the downregulation of cell surface MHC-I by the HIV-encoded accessory protein Nef, suggesting a possible therapeutic role of Concanamycin A in enhancing the immune-mediated clearance of HIV-infected cells (5).
- Kinashi, H. et al. (1984) J Antibiot (Tokyo) 37, 1333-43.
- Jefferies, K.C. et al. (2008) Arch Biochem Biophys 476, 33-42.
- Nishihara, T. et al. (1995) Biochem Biophys Res Commun 212, 255-62.
- Hong, J. et al. (2006) J Pharmacol Exp Ther 319, 672-81.
- Painter, M.M. et al. (2020) Proc Natl Acad Sci U S A 117, 23835-23846.
Molecular Formula
C46H75NO14
Molecular Weight
866.1 g/mol
Purity
>98%
CAS
80890-47-7
Solubility
Soluble in DMSO at 50 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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