1,3-Bis(N-carbobenzoyloxy-L-leucyl)amino Acetone
1,3-Bis(CBZ-Leu-NH)-2-propanone Off-white lyophilized solid. PACKAGED UNDER INERT GAS. A cell-permeable, symmetrical bis(acylamino)ketone that acts as a potent, selective, and reversible inhibitor of cathepsin K (Ki,app = 22 nM). Shown to bind to cathepsin K and span both the S- and S′-subsites. A poor inhibitor of papain (Ki,app > 10 µM) but displays greater selectivity towards other proteases of the papain family (Ki,app = 340 nM, 890 nM, and 1.3 µM for cathepsin L, cathepsin S, and cathepsin B respectively). Inhibits trypsin and chymotrypsin activities only at higher concentrations (Ki,app ≥ 50 µM). Purity: ≥95% by HPLC. Cbz-Leu-NH-CH2-CO-CH2-NH-Leu-Cbz Ref.: Claveau, D., et al. 2000. Biochem. Pharmacol. 60, 759. LaLonde, J.M., et al. 1999. Biochemistry 38, 862. Yamashita, D.S., et al. 1997. J. Am. Chem. Soc. 119, 11351. |
