White solid. PROTECT FROM LIGHT. A macrolide antibiotic that acts as a specific inhibitor of vacuolar-type H+-ATPase (V-type; Ki = 500 pM). A valuable tool for distinguishing among different types of ATPases. Blocks lysosomal cholesterol trafficking in macrophages and is known to interfere with pH regulation in brain cells. Exhibits cytotoxic effects on a number of cell lines in a cell viability assay. Reported to selectively inhibit b-secretase, an enzyme involved in the processing of amyloid precursor protein (APP). Purity: ≥95% by HPLC. CAS 88899-55-2. Ref.: Sinha, S., and Lieberburg, I. 1999. Proc. Natl. Acad. Sci. USA 96, 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. Biochemistry 32, 3902. Furuchi, T., et al. 1993. J. Biol. Chem. 268, 27345. Bowman, E.J., et al. 1988. Proc. Natl. Acad. Sci. USA 85, 7972.
R: 36/37/38; S: 22-26-36 |
