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MG-132 is a potent, reversible and cell permeable proteasome inhibitor. The ubiquitin-proteasome pathway plays an integral role in the selective degradation of intracellular proteins. While important for clearing damaged or misfolded proteins, this proteolytic pathway also regulates the availability of key proteins involved in the control of inflammatory processes, cell cycle regulation, and gene expression.

MG-132 inhibits 5-lipoxygenase which selectively disrupts c-Myc function in cancer cells. MG-132 also inhibits NF-κB activation.

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