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Proteasome Inhibitor II is a potent, cell-permeable, reversible proteasome inhibitor. The compound has been shown to inhibit chymotrypsin-like activity of the pituitary multicatalytic proteinase complex (MPC; Ki = 460 nM). Proteasome Inhibitor II blocks the decay of IkB-a and IkB-b proteins in exponentially growing WEHI 231 cells. The chemical has been shown not to inhibit the peptidyl-glutamyl peptide hydrolyzing activity of MPC at concentrations as high as 200 µM.
1. Orlowski, M., et al., 1993. Evidence for the presence of five distinct proteolytic components in the pituitary multicatalytic proteinase complex. Properties of two components cleaving bonds on the carboxyl side of branched chain and small neutral amino acids. Biochemistry. 32(6): 1563-72. PMID: 8431436
2. Orlowski, M., et al., 1997. Reactions of [14C]-3,4-dichloroisocoumarin with subunits of pituitary and spleen multicatalytic proteinase complexes (proteasomes). Biochemistry. 36(45): 13946-53. PMID: 9374874
3. Schauer, S L., et al., 1998. Dominant signals leading to inhibitor kappaB protein degradation mediate CD40 ligand rescue of WEHI 231 immature B cells from receptor-mediated apoptosis. Journal of immunology (Baltimore, Md. : 1950). 160(9): 4398-405. PMID: 9574544
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