Drug intelligence / Profile preview

mg132

Development stage
Preclinical
Modality
Small Molecules, Peptides
Administration
In Vitro, Intraperitoneal (in Animal Models)
01

Overview

MG132 is a potent, reversible, and cell-permeable proteasome inhibitor that specifically blocks the chymotrypsin-like activity of the 26S proteasome complex. By inhibiting proteasomal degradation, MG132 leads to the accumulation of polyubiquitinated proteins, thus modulating numerous cellular pathways including apoptosis, cell cycle regulation, and inflammatory signaling. It also inhibits calpain and suppresses NF-κB activation by preventing IκB degradation. MG132 exhibits anti-cancer effects by inducing cell cycle arrest and apoptosis, and has been explored in preclinical research for its ability to sensitize cancer cells to chemotherapeutic agents and induce anti-tumor effects in various models. MG132 is primarily used as a research tool in cellular and molecular biology; it is not approved for clinical use[3][4][5][8][9][10].

Other names
carbobenzyloxy-leucinyl-leucinyl-leucinalN-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinalbenzyl N-((2S)-4-methyl-1-(((2S)-4-methyl-1-(((2S)-4-methyl-1-oxopentan-2-yl)amino)-1-oxopentan-2-yl)amino)-1-oxopentan-2-yl)carbamateProteasome Inhibitor MG-132Z-LLL-CHOZ-LL-CHOZ-LLL-alZ-Leu-Leu-Leu-CHO
02

Targets

CAPN (Schistosoma calpain large subunit family)26S proteasome

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