|Molecular Weight||866.1 g/mol|
|Solubility||Soluble in DMSO at 50 mg/mL.|
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).
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