Calpain Inhibitor I
LLNL
MG 101 White to off-white solid. Cell-permeable inhibitor of calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM). Inhibits neutral cysteine proteases and the proteasome (Ki = 6 µM). Modulates the processing of the b-amyloid precursor protein (bAPP) to b-amyloid (Ab). Protects against neuronal damage caused by hypoxia and ischemia. Inhibits apoptosis in thymocytes and metamyelocytes. Also inhibits reovirus-induced apoptosis in L929 cells. Inhibits the proteolysis of IkB-a and IkB-b by the ubiquitin-proteasome complex. Inhibits cell cycle progression at G1/S and metaphase/anaphase in CHO cells by inhibiting cyclin B degradation. Also prevents nitric oxide production by activated macrophages by interfering with transcription of the inducible nitric oxide synthase gene. Purity: ≥95% by HPLC. CAS 110044-82-1. N-Acetyl-Leu-Leu-Nle-CHO Ref.: Debiasi, R.L., et al. 1999. J. Virol. 73, 695. Zhang, L., et al. 1999. J. Biol. Chem. 274, 8966. Milligan, S.A., et al. 1996. Arch. Biochem. Biophys. 335, 388. Griscavage, J.M., et al. 1995. Biochem. Biophys. Res. Commun. 215, 721. Squier, M.K., et al. 1994. J. Cell Physiol. 159, 229. Rami, J., and Kreiglstein, J. 1993. Brain Res. 609, 67. Sherwood, S.W., et al. 1993. Proc. Natl. Acad. Sci. USA 90, 3353. Vinitsky, A., et al. 1992. Biochemistry 31, 9421. Sasaki, T., et al. 1990. J. Enzyme Inhib. 3, 195. |
