CX-5461/CX5461/

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

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]

参考文献

[1] http://en.wikipedia.org/wiki/MG132

[2] Steinhilb ML et al. J Biol Chem. 2001 Feb 9;276(6):4476-84.

[3] Tsubuki S et al. J Biochem. 1996 Mar;119(3):572-6.