MG132

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MG132
MG132.svg
Names
IUPAC name
Benzyl 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]carbamate
Other names
N-Benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal
Z-Leu-Leu-Leu-al
Identifiers
3D model (JSmol)
ChemSpider
Properties
C26H41N3O5
Molar mass 475.63 g·mol−1
Appearance White solid
Solubility 100 mM in EtOH and DMSO
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references

MG132 is a potent, reversible, and cell-permeable proteasome inhibitor [1] (Ki = 4 nM). It belongs to the class of synthetic peptide aldehydes [2]. 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. MG132 activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis. MG132 also inhibits NF-κB activation with an IC50 of 3 µM and prevents β-secretase cleavage.

References[edit]

  1. ^ Hayashi M, Saito Y, Kawashima S (Jan 31, 1992). "Calpain activation is essential for membrane fusion of erythrocytes in the presence of exogenous Ca2+". Biochem Biophys Res Commun. 182 (2): 939–946. PMID 1734892. 
  2. ^ Ito A, Takahashi R, Muira C, Baba Y (1975). "Synthetic Study of Peptide Aldehydes". Chemical and Pharmaceutical Bulletin. 12 (23): 2106–3113. doi:10.1248/cpb.37.3229. PMID 8987871.