Chemical Name:N-Benzyloxycarbonyl-L-leucylnorleucinal
Biological Activity:
Potent, cell-permeable inhibitor of the Ca2+-dependent
protease, calpain. Prevents collagen- and thrombin-induced platelet
aggregation, probably by blocking calpain induced phospholipase C and
thromboxane synthase activation. Potent cathepsin L inhibitor. Recently shown
to preferentially inhibit a subset of protein-tyrosine phosphatases.
Tsujinakaet al (1988) Synthesis of a new cell penetrating calpain
inhibitor (calpeptin). Biochem.Biophys.Res.Comm. 153 1201. Sasakiet al (1990) Inhibitory effect of di-and tripeptidyl aldehydes
on calpains and cathepsins. J.Enz.Inhib. 3 195. Mehdi
(1991) Cell-penetrating inhibitors of calpain. TiBS 16 150. Schoenwaelder
and Burridge (1999) Evidence for a calpeptin-sensitive protein-tyrosine
phosphatase upstream of the small GTPase Rho. J.Biol.Chem. 274
14359.
