Description |
Chemical Name: (3 Z ,5 E ,7 R ,8 S ,9 S ,11 E ,13 E ,15 S ,16 R )-8-Hydroxy-16-[(1 S ,2 R ,3 S )-2-hydroxy-1-methyl-3-[(2 R ,4 R ,5 S ,6 R )-tetrahydro-2,4-dihydroxy-5-methyl-6-(1-methylethyl)-2 H -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 (IC 50 = 0.6 - 1.5 nM in bovine chromaffin granules). Selective for v-ATPase over other ATP hydrolyzing enzymes such as F-ATPases and the H + /K + -ATPase (P-ATPase). Thought to inhibit autophagy either by blocking autophagosome-lysosome fusion (in H4IIE cells), or by blocking lysosomal degradation.
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