MG132 is a potent, reversible, and cell-permeable proteasome inhibitor [1] (K i = 4 nM). It belongs to the class of synthetic peptide aldehydes. [2] [3] It 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.

Aug 31, 2016 · MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50 s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis. For research use only. We do not sell to patients.

2 days ago · MG-132 is a potent proteasome and calpain inhibitor. Research studies have shown that MG-132 prevents degradation of the proteasome substrates SucLLVY-MCA and ZLLL-MCA with an IC 50 of 850 nM and 100 nM, respectively, as well as inhibits casein-degrading activity of m-calpain with an IC 50 of 1.25 µM (1).

In this study, we investigated the in vitro effects of the proteasome inhibitor MG132 on the release of TNF-α, IL-1β and IL-6 and their receptors, as well as on the activation of NF-κB and AP-1 and the inhibitor of the NF-κB (IκB) degradation, in the monocyte/macrophage-derived cell line U937.

We found that MG132 could effectively reverse skeletal muscle atrophy and inhibit tumor growth, accompanied by downregulation of the NF-κB/ubiquitin–proteasome pathway. MG132 is a potent and reversible proteasome inhibitor whose clinical implications have been studied extensively.

MG132 can significantly enhance the sensitivity of esophageal cancer cells to cisplatin and effectively improve the rate of cell apoptosis by inhibiting the activation of NF-κB, potentiating the expression levels of apoptosis-related protein caspase-8 and -3.

Apr 6, 2022 · Rat pheochromocytoma (PC12) cells were treated with the proteasome inhibitor MG-132 and morphological changes were recorded. Initially, neuronal differentiation was induced but after 24 h signs...

MG132 is a potent proteasome inhibitor that also inhibits calpains and lysosomal cathepsins. One of the first proteasome inhibitors to be developed, MG-132 is widely used in proteasome inhibition studies because of its high potency, high selectivity, and rapid reversibility. MG132 mechanistically acts as a proteasome inhibitor by hemiacetal ...

MG-132 is a peptide aldehyde (Z-Leu-Leu-Leu-al) that selectively blocks the proteolytic activity of the 26S proteasome. The 26S proteasome is a large protease complex that degrades ubiquitinated proteins into smaller peptides. It plays a central role in the regulation of proteins that control cell-cycle progression and apoptosis. More details.