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Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Chemical compound
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.
^Lee, Do Hee; Goldberg, Alfred L (October 1998). "Proteasome inhibitors: valuable new tools for cell biologists". Trends in Cell Biology. 8 (10): 397–403. doi:10.1016/S0962-8924(98)01346-4. PMID 9789328.
^Ito A, Takahashi R, Muira C, Baba Y (1975). "Synthetic Study of Peptide Aldehydes". Chemical and Pharmaceutical Bulletin. 12 (23): 3106–3113. doi:10.1248/cpb.23.3106.
^Hayashi M, Saito Y, Kawashima S (31 January 1992). "Calpain activation is essential for membrane fusion of erythrocytes in the presence of exogenous Ca2+". Biochem Biophys Res Commun. 182 (2): 939–946. doi:10.1016/0006-291x(92)91822-8. PMID 1734892.
MG132 is a potent, reversible, and cell-permeable proteasome inhibitor (Ki = 4 nM). It belongs to the class of synthetic peptide aldehydes. It reduces...
and MG132, are artificially synthesized and retain their protecting groups, which have specific codes. Bortezomib is Pyz–Phe–boroLeu, and MG132 is Z–Leu–Leu–Leu–al...
of protease: an amino-terminal threonine protease. Bortezomib (Boronated MG132), a molecule developed by Millennium Pharmaceuticals and marketed as Velcade...
clinical trials. Epoxomicin is a naturally occurring selective inhibitor. MG132 is a synthesized peptide commonly used for in vitro studies. Beta-hydroxy...
cycle. Molecularly, It has been proposed that proteasome inhibition by MG132 can stabilize Runx2 protein levels in late G1 and S in MC3T3 cells, but...
degradation for a protein substrate of interest. Drug treatments (such as MG132) are also used to inhibit steps of degradation, followed by a cycloheximide...
"Engineering and In Vitro Evaluation of Acid Labile Cholesterol Tethered MG132 Nanoparticle for Targeting Ubiquitin-Proteasome System in Cancer". ChemistrySelect...
from degradation, such as in the presence of proteasome inhibitors like MG132, the mitotic exit induced by flavopiridol can be reversed. This finding...
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