![]() | This article includes a list of general
references, but it lacks sufficient corresponding
inline citations. (November 2015) |
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Names | |
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Systematic IUPAC name
Benzyl [(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)
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ChemSpider | |
PubChem
CID
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UNII | |
CompTox Dashboard (
EPA)
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Properties | |
C26H41N3O5 | |
Molar mass | 475.630 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).
|
MG132 is a potent, reversible, and cell-permeable proteasome inhibitor [1] ( Ki = 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. 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.
There are several inhibitors that can readily enter cell and selectively inhibit degradative pathway. It includes peptide aldehydes, such as Cbz-leu-leu-leucinal (MG132), Cbz-leu-leu-norvalinal ( MG115) and acetyl-leu-leu-norleucinal ( ALLN). [1] These are substrate analogues and potent transition-state inhibitors of chymotrypsin like activity of proteasome machinery. [4] [5] The peptide aldehydes are also known to inhibit certain lysosomal cysteine proteases and the calpains hence MG132 may not be exclusive inhibitor of proteasomal pathway. [4]
![]() | This article includes a list of general
references, but it lacks sufficient corresponding
inline citations. (November 2015) |
![]() | |
Names | |
---|---|
Systematic IUPAC name
Benzyl [(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 | |
PubChem
CID
|
|
UNII | |
CompTox Dashboard (
EPA)
|
|
| |
| |
Properties | |
C26H41N3O5 | |
Molar mass | 475.630 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).
|
MG132 is a potent, reversible, and cell-permeable proteasome inhibitor [1] ( Ki = 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. 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.
There are several inhibitors that can readily enter cell and selectively inhibit degradative pathway. It includes peptide aldehydes, such as Cbz-leu-leu-leucinal (MG132), Cbz-leu-leu-norvalinal ( MG115) and acetyl-leu-leu-norleucinal ( ALLN). [1] These are substrate analogues and potent transition-state inhibitors of chymotrypsin like activity of proteasome machinery. [4] [5] The peptide aldehydes are also known to inhibit certain lysosomal cysteine proteases and the calpains hence MG132 may not be exclusive inhibitor of proteasomal pathway. [4]