Biochem/physiol Actions
Primary Targetvacuolar-type H+-ATPase
Cell permeable: yes
General description
A macrolide antibiotic that acts as a specific inhibitor of vacuolar-type H+-ATPase (V-type; Ki = 0.5 nM) and is a valuable tool for distinguishing among different types of ATPases. Reported to selectivity inhibit β-secretase, an enzyme involved in the processing of amyloid precursor protein (APP). Blocks lysosomal cholesterol trafficking in macrophages. Known to interfere with pH regulation in brain cells. Inhibits bone resorption both in vivo and in vitro. Has been shown to exhibit cytotoxic effects on a number of cell lines in a cell viability assay.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Sinha, S., and Lieberburg, I. 1999. Proc. Natl. Acad. Sci. USA96, 11049.Calvert, C.M., and Sanders, D. 1995. J. Biol. Chem.270, 7272.Nishihara, T., et al. 1995. Biochem. Biophys. Res. Commun.269, 255.Crider, B.P., et al. 1994. J. Biol. Chem.269, 17379.Palokangas, H., et al. 1994. J. Biol. Chem.269, 17577.Sundquist, K.T., and Marks, S.C., Jr. 1994. J. Bone Miner. Res.9, 1575.Drose, S., et al. 1993. Biochemistry32, 3902.Furuchi, T., et al. 1993. J. Biol. Chem.268, 27345.Bowman, E.J., et al. 1988. Proc. Natl. Acad. Sci. USA85, 7972.
Packaging
Packaged under inert gas
15 µg in Glass bottle
Reconstitution
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 1 year at -20°C. Use only fresh DMSO for further dilutions.
Warning
Toxicity: Standard Handling (A)
This product has met the following criteria: