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Bafilomycin A1
Chemical Name:(3Z,5E,7R,8S,9S,11E,13E,15S,16R)-8-Hydroxy-16-[(1S,2R,3
S)-2-hydroxy-1-methyl-3-[(2R,4R,5S,6R)-tetrahydro-2,4-d
ihydroxy-5-methyl-6-(1-methylethyl)-2H-pyran-2-yl]butyl
]-3,15-dimethoxy-5,7,9,11-tetramethyloxacyclohexadeca-3
,5,11,13-tetraen-2-one
Biological Activity:
Highly potent, selective inhibitor of vacuolar H+-ATPases
(IC50 = 500 pM as measured in chromaffin granule membranes).
Selective over other ATP hydrolyzing enzymes such as F-ATPases, Ca2+-ATPases,
Na+/K+-ATPases and plasma membrane H+-ATPases.
Bowmanet al (1988) Bafilomycins: a class of inhibitors of
membrane ATPases from microorganisms, animal cells, and plant cells.
Proc.Natl.Acad.Sci.USA 85 7972.Palokangaset al (1998) Retrograde transport from the
pre-golgi complex is affected by the vacuolar H+-ATPase inhibitor
bafilomycin A1. Mol.Biol.Cell 8 3561. Gagliardiet al
(1999) Chemistry and stucture activity relationships of bafilomycin A1, a potent and selective
inhibitor of the vacuolar H+-ATPase. Curr.Med.Chem. 6 1197.
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