Chemical Name: N-[(Phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide
Biological ActivityMG 132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM). MG 132 inhibits TNF-α-induced NF-κB activation and IκBα degradation. Induces neurite outgrowth in PC12 cells and has anticancer properties in vitro. MG 132 inhibits SARS-CoV-2 Mpro in vitro (IC50 = 3.9 μM) and inhibits viral replication. Also enhances adeno-associated viral transduction efficiency of human cell lines by around 50-fold.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Potential of the proteasome inhibitor MG-132 as an anticancer agent, alone and in combination.
Banerjee and Liefshitz
Anticancer Res., 2001;21:3941
The ubiquitin-proteasome pathway is required for processing the NF-κB1 precursor protein and the activation of NF-κB.
Palombella et al.
Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-Leucine and tri-Leucine.
Tsubuki et al.
Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease.
Ma et al.
Cell Res., 2020;
Intracellular trafficking of adeno-associated virus vectors: routing to the late endosomal compartment and proteasome degradation
Douar et al.
Citations for MG 132
The citations listed below are publications that use Tocris products. Selected citations for MG 132 include:
60 Citations: Showing 1 - 10
Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells
Authors: Kaji Et al.
Sci Rep 2020;10:3088
MARK2/Par1b kinase present at centrosomes and retraction fibres corrects spindle off-centring induced by actin disassembly.
Authors: Hart Et al.
Open Biol 2019;9:180263
Miro proteins prime mitochondria for Parkin translocation and mitophagy.
Authors: Safiulina Et al.
EMBO J 2019;38
Lethal Poisoning of Cancer Cells by Respiratory Chain Inhibition plus Dimethyl α-Ketoglutarate.
Authors: Sica Et al.
Cell Rep 2019;27:820
Co-targeting RNA Polymerases IV and V Promotes Efficient De Novo DNA Methylation in Arabidopsis.
Authors: Gallego-Bartolomé Et al.
Gigaxonin E3 ligase governs ATG16L1 turnover to control autophagosome production.
Authors: Scrivo Et al.
Nat Commun 2019;10:780
Post-translational regulation of lipogenesis via AMPK-dependent phosphorylation of ins.-induced gene.
Authors: Han Et al.
Nat Commun 2019;10:623
Epigenetic control of IL-23 expression in keratinocytes is important for chronic skin inflammation.
Authors: Li Et al.
Nat Commun 2018;9:1420
Spindle rotation in human cells is reliant on a MARK2-mediated equatorial spindle-centering mechanism.
Authors: Zulkipli Et al.
J Cell Biol 2018;217:3057
Serine protease modulation of Dependence Receptors and EMT protein expression.
Authors: McNair Et al.
Cancer Biol Ther 2018;20:349
27-Hydroxycholesterol increases α-synuclein protein levels through proteasomal inhibition in human dopaminergic neurons.
Authors: Schommer Et al.
BMC Neurosci 2018;19:17
Loss of the novel Vcp (valosin containing protein) interactor Washc4 interferes with autophagy-mediated proteostasis in striated muscle and leads to myopathy in vivo.
Authors: Kustermann Et al.
Capsaicin-induced TRIB3 upregulation promotes apoptosis in cancer cells.
Authors: Lin Et al.
Cancer Manag Res 2018;10:4237
TRAF3IP2 mediates high glucose-induced endothelin-1 production as well as endothelin-1-induced inflammation in endothelial cells.
Authors: Padilla Et al.
Am J Physiol Heart Circ Physiol 2017;:ajpheart.00478.2017
Aurora-B kinase pathway controls the lateral to end-on conversion of kinetochore-microtubule attachments in human cells.
Nat Commun 2017;8(1):150
Ubiquitin ligase SYVN1/HRD1 facilitates degradation of the SERPINA1 Z variant/α-1-antitrypsin Z variant via SQSTM1/p62-dependent selective autophagy.
Authors: Feng Et al.
Noncanonical SQSTM1/p62-Nrf2 pathway activation mediates proteasome inhibitor resistance in multiple myeloma cells via redox, metabolic and translational reprogramming.
Authors: Riz Et al.
Analogs of the novel phytohormone, strigolactone, trigger apoptosis and synergize with PARP inhibitors by inducing DNA damage and inhibiting DNA repair.
Authors: Croglio Et al.
Atrogin-1 Deficiency Leads to Myopathy and Heart Failure in Zebrafish.
Authors: Bühler Et al.
Int J Mol Sci 2016;17
Glycogen Synthase Kinase-3β and Caspase-2 Mediate Ceramide- and Etoposide-Induced Apoptosis by Regulating the Lysosomal-Mitochondrial Axis.
Authors: Lin Et al.
J Cell Sci 2016;11:e0145460
A sensitised RNAi screen reveals a ch-TOG genetic interaction network required for spindle assembly.
Authors: Barr and Bakal
J Neurosci 2015;5:10564
A proteomic study of mitotic phase-specific interactors of EB1 reveals a role for SXIP-mediated protein interactions in anaphase onset.
Authors: Tamura Et al.
Biol Open 2015;4:155
Estrogen receptor alpha mediates epithelial to mesenchymal transition, expression of specific matrix effectors and functional properties of breast cancer cells.
Authors: Bouris Et al.
Matrix Biol 2015;43:42
Extracellular glutamate exposure facilitates group I mGluR-mediated epileptogenesis in the hippocampus.
Authors: Zhao Et al.
Respir Res 2015;35:308
The E3 ubiquitin ligase ARIH1 protects against genotoxic stress by initiating a 4EHP-mediated mRNA translation arrest.
Authors: Stechow Et al.
PLoS One 2015;35:1254
Decreased expression of the NF-κB family member RelB in lung fibroblasts from Smokers with and without COPD potentiates cigarette smoke-induced COX-2 expression.
Authors: Sheridan Et al.
Mol Cell Biol 2015;16:54
SILAC-Based Mass Spectrometry Analysis Reveals That Epibrassinolide Induces Apoptosis via Activating Endoplasmic Reticulum Stress in Prostate Cancer Cells.
Authors: Obakan Et al.
PLoS One 2015;10:e0135788
Up-regulation of TREK-2 potassium channels in cultured astrocytes requires de novo protein synthesis: relevance to localization of TREK-2 channels in astrocytes after transient cerebral ischemia.
Authors: Rivera-Pagán Et al.
PLoS One 2015;10:e0125195
Translational initiation regulated by ATM in dendritic cells development.
Cell Death Dis 2014;5:e1418
Single nucleotide polymorphism-specific regulation of matrix metalloproteinase-9 by multiple miRNAs targeting the coding exon.
Authors: Duellman Et al.
Nucleic Acids Res 2014;42:5518
HSF1 deficiency and impaired HSP90-dependent protein folding are hallmarks of aneuploid human cells.
Authors: Donnelly Et al.
EMBO J 2014;33:2374
Methyllysine reader plant homeodomain (PHD) finger protein 20-like 1 (PHF20L1) antagonizes DNA (cytosine-5) methyltransferase 1 (DNMT1) proteasomal degradation.
Authors: Estève Et al.
J Biol Chem 2014;289:8277
Phosphorylation and degradation of tomosyn-2 de-represses Ins secretion.
Authors: Bhatnagar Et al.
J Biol Chem 2014;289:25276
Regulation of YAP by mTOR and autophagy reveals a therapeutic target of tuberous sclerosis complex.
Authors: Liang Et al.
Cell Cycle 2014;211:2249
Mammalian target of rapamycin complex 2 modulates αβTCR processing and surface expression during thymocyte development.
Authors: Chou Et al.
J Immunol 2014;193:1162
Halofuginone-induced amino acid starvation regulates Stat3-dependent Th17 effector function and reduces established autoimmune inflammation.
Authors: Carlson Et al.
J Immunol 2014;192:2167
BECN1 is involved in the initiation of mitophagy: it facilitates PARK2 translocation to mitochondria.
Authors: Choubey Et al.
Arkadia regulates tumor metastasis by modulation of the TGF-β pathway.
Authors: Briones-Orta Et al.
PLoS One 2013;73:1800
A critical role for protein degradation in the nucleus accumbens core in cocaine reward memory.
Authors: Ren Et al.
Proteasomal degradation of eukaryotic elongation factor-2 kinase (EF2K) is regulated by cAMP-PKA signaling and the SCFβTRCP ubiquitin E3 ligase.
Authors: Wiseman Et al.
J Biol Chem 2013;288:17803
Drosophila SOCS36E negatively regulates JAK/STAT pathway signaling via two separable mechanisms.
Authors: Stec Et al.
Mol Biol Cell 2013;24:3000
Lateral to end-on conversion of chromosome-microtubule attachment requires kinesins CENP-E and MCAK.
Authors: Shrestha and Draviam
Curr Biol 2013;23:1514
Human bocavirus VP2 upregulates IFN-β pathway by inhibiting ring finger protein 125-mediated ubiquitination of retinoic acid-inducible gene-I.
Authors: Luo Et al.
J Immunol 2013;191:660
Autophagy-mediated turnover of dynamin-related protein 1.
Authors: Purnell and Fox
BMC Neurosci 2013;14:86
Automated tracking of mitotic spindle pole positions shows that LGN is required for spindle rotation but not orientation maintenance.
Authors: Corrigan Et al.
Eur J Neurosci 2013;12:2643
Spatiotemporal organization of Aurora-B by APC/CCdh1 after mitosis coordinates cell spreading through FHOD1.
Authors: Floyd Et al.
J Appl Physiol (1985) 2013;126:2845
Molecular mechanism of mutant p53 stabilization: the role of HSP70 and MDM2.
Authors: Wiech Et al.
PLoS One 2012;7:e51426
On the mechanism of synaptic depression induced by CaMKIIN, an endogenous inhibitor of CaMKII.
Authors: Gouet Et al.
PLoS One 2012;7:e49293
Tgf-β induced Erk phosphorylation of smad linker region regulates smad signaling.
Authors: Hough Et al.
PLoS One 2012;7:e42513
Free fatty acid palmitate impairs the vitality and function of cultured human bladder smooth muscle cells.
Authors: Oberbach Et al.
Proc Natl Acad Sci U S A 2012;7:e41026
Reversible modification of adenomatous polyposis coli (APC) with K63-linked polyubiquitin regulates the assembly and activity of the β-catenin destruction complex.
Authors: Tran and Polakis
J Biol Chem 2012;287:28552
Punctuated cyclin synthesis drives early embryonic cell cycle oscillations.
Mol Biol Cell 2012;23:284
Quantitative profiling of caspase-cleaved substrates reveals different drug-induced and cell-type patterns in apoptosis.
Authors: Shimbo Et al.
Stem Cells 2012;109:12432
Macrophage migration inhibitory factor promotes cell death and aggravates neurologic deficits after experimental stroke.
Authors: Inácio Et al.
J Cereb Blood Flow Metab 2011;31:1093
Epigenetic centromere specification directs aurora B accumulation but is insufficient to efficiently correct mitotic errors.
Authors: Bassett Et al.
Sci Rep 2010;190:177
N-MthD.-aspartate receptor- and metabotropic glutamate receptor-dependent long-term depression are differentially regulated by the ubiquitin-proteasome system.
Authors: Citri Et al.
Cancer Res 2009;30:1443
Leptin enhances synthesis of proinflammatory mediators in human osteoarthritic cartilage--mediator role of NO in leptin-induced PGE2, IL-6, and IL-8 production.
Authors: Vuolteenaho Et al.
Mediators Inflamm 2009;2009:345838
The effect of denervation on protein synthesis and degradation in adult rat diaphragm muscle.
Authors: Argadine Et al.
J Exp Med 2009;107:438
Calcineurin-mediated dephosphorylation of c-Jun Ser-243 is required for c-Jun protein stability and cell transformation.
Authors: Huang Et al.
Effects of levo- and dextrosimendan on NF-kappaB-mediated transcription, iNOS expression and NO production in response to inflammatory stimuli.
Authors: Sareila Et al.
Br J Pharmacol 2008;155:884
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