• Catalog Number:

  E1KS2619

• Amount:

  5mg1​ PHYSICAL AND CHEMICAL PROPERTIES

2​ Biological Activity MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50 of 0.1 and 1.2 μM for the inhibition of proteasome and calpain, respectively. The Ki of MG132 is 4 nM. MG132 inhibits TNF-α-induced NF-κB activation and IκBα degradation with an IC50 of 3 µM and prevents β-secretase cleavage. MG132 induces neurite outgrowth in PC12 cells and has anticancer properties in vitro. MG132 reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable strains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. MG132 activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis. [1][2][3] 3​ References: Differential Inhibition of Calpain and Proteasome Activities by Peptidyl Aldehydes of Di-Leucine and Tri-Leucine Satoshi Tsubuki,Yumiko Saito,et al. J. Biochem 1996;119:, 572-576 http://en.wikipedia.org/wiki/MG132 http://en.wikipedia.org/wiki/MG132 ; The protease inhibitor, MG132, blocks maturation of the amyloid precursor protein Swedish mutant preventing cleavage by beta-Secretase. Steinhilb ML et al. J BiolChem. 2001 Feb 9;276(6):4476-84. The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.