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Calpain Inhibitor II is a cell-permeable, peptide aldehyde inhibitor of calpain I (Ki=190nM), calpain II (C-1259)(Ki=150nM), cathepsin B, cathepsin L (Ki=0.5nM) and other neutral cysteine proteases. Calpain Inhibitor II inhibits cell cycle progression at G1/S and metaphase/anaphase in CHO cells by inhibiting cyclin B degradation. Also stimulates HMG-CoA synthase transcription by inhibiting degradation of active SREBP-1 (sterol regulatory element-binding protein 1). Protects against neuronal damage caused by hypoxia and ischemia.

Calpain Inhibitor II inhibits apoptosis in thymocytes and metamyelocytes. Also prevents nitric oxide production by activated macrophages by interfering with the transcription of inducible nitric oxide synthase (iNOS; NOS II). Inhibits proteolytic degradation of IκBα and IκBß in RAW macrophages induced with LPS. It also prolong association of MHC class I molecules with the transporters associated with antigen processing.

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