MG-132

外観

白色～うすい褐色、結晶～粉末白色～うすい褐色, 結晶～粉末

溶解性

エタノールに可溶

用途

ユビキチン-プロテアソーム系研究用。

使用上の注意

不活性ガス封入

使用

A proteasome and NF-κB inhibitor.

定義

ChEBI: A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative.

一般的な説明

Potent, reversible, and cell-permeable proteasome inhibitor (K_i = 4 nM). Reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable stains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. Activates c-Jun N-terminal kinase (JNK1) and inhibits NF-κB activation (IC₅₀ = 3 μM).

生物活性

Potent cell-permeable inhibitor of proteasome (IC 50 = 100 nM) and calpain (IC 50 = 1.2 μ M). Inhibits TNF- α -induced NF- κ B activation and I κ B α degradation. Induces neurite outgrowth in PC12 cells and has anticancer properties in vitro .