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Description: Proteasome and calpain inhibitor. Inhibits NF-κB activation
Alternative Names: Z-LLL-al,Z-Leu-Leu-Leu-CHO
Chemical Name: N-[(Phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide
Purity: ≥95% (HPLC)
Biological Activity for MG 132
MG 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.
Technical Data for MG 132
| M. Wt | 475.63 |
| Formula | C26H41N3O5 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 133407-82-6 |
| PubChem ID | 90488707 |
| InChI Key | AUQBNOXQYSNYAH-OJSMNCEXSA-N |
| Smiles | [H]C(C)C[C@H](NC(=O)OCC1=CC=CC=C1)C(=O)NC(CC(C)C)C(=O)N[C@@H](CC(C)C)C(C)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for MG 132
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 47.56 | 100 | |
| DMSO | 47.56 | 100 |
Preparing Stock Solutions for MG 132
The following data is based on the product molecular weight 475.63. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.1 mL | 10.51 mL | 21.02 mL |
| 5 mM | 0.42 mL | 2.1 mL | 4.2 mL |
| 10 mM | 0.21 mL | 1.05 mL | 2.1 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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Product Datasheets for MG 132
References for MG 132
References are publications that support the biological activity of the product.
Banerjee and Liefshitz (2001) Potential of the proteasome inhibitor MG-132 as an anticancer agent, alone and in combination. Anticancer Res. 21 3941 PMID: 11911275
Palombella et al (1994) The ubiquitin-proteasome pathway is required for processing the NF-κB1 precursor protein and the activation of NF-κB. Cell 78 773 PMID: 8087845
Tsubuki et al (1996) Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-Leucine and tri-Leucine. J.Biochem. 119 572 PMID: 8830056
Ma et al (2020) Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease. Cell Res. 30 678 PMID: 32541865
Douar et al (2001) Intracellular trafficking of adeno-associated virus vectors: routing to the late endosomal compartment and proteasome degradation J.Virol. 75 1824 PMID: 11160681
If you know of a relevant reference for MG 132, please let us know.
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Keywords: MG 132, MG 132 supplier, Proteasome, calpain, inhibitors, inhibits, NF-κB, NF-kappaB, NF-kB, activation, Transcription, Factors, Nuclear, Factor, Kappa, B, Proteinases, Proteases, Ca2+Sensitive, Protease, modulators, Calcium-Sensitive, MG132, anticancer, viral, transduction, enhancers, enhances, SARS, Z-LLL-al, Z-Leu-Leu-Leu-CHO, Calpains, NF-kB/IkB, 3C, and, 3CL, Viral, Transduction, Enhancers, 1748, Tocris Bioscience
60 Citations for MG 132
Citations are publications that use Tocris products. Selected citations for MG 132 include:
Bühler et al (2016) Atrogin-1 Deficiency Leads to Myopathy and Heart Failure in Zebrafish. Int J Mol Sci 17 PMID: 26840306
Riz et al (2016) Noncanonical SQSTM1/p62-Nrf2 pathway activation mediates proteasome inhibitor resistance in multiple myeloma cells via redox, metabolic and translational reprogramming. Oncotarget 7 66360 PMID: 27626179
Croglio et al (2016) Analogs of the novel phytohormone, strigolactone, trigger apoptosis and synergize with PARP inhibitors by inducing DNA damage and inhibiting DNA repair. Oncotarget 7 13984 PMID: 26910887
Zhao et al (2015) Extracellular glutamate exposure facilitates group I mGluR-mediated epileptogenesis in the hippocampus. Respir Res 35 308 PMID: 25568123
Sheridan et al (2015) 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. Mol Cell Biol 16 54 PMID: 25943190
Stechow et al (2015) The E3 ubiquitin ligase ARIH1 protects against genotoxic stress by initiating a 4EHP-mediated mRNA translation arrest. PLoS One 35 1254 PMID: 25624349
Wiech et al (2012) Molecular mechanism of mutant p53 stabilization: the role of HSP70 and MDM2. PLoS One 7 e51426 PMID: 23251530
Tran and Polakis (2012) Reversible modification of adenomatous polyposis coli (APC) with K63-linked polyubiquitin regulates the assembly and activity of the β-catenin destruction complex. J Biol Chem 287 28552 PMID: 22761442
Carlson et al (2014) Halofuginone-induced amino acid starvation regulates Stat3-dependent Th17 effector function and reduces established autoimmune inflammation. J Immunol 192 2167 PMID: 24489094
Sica et al (2019) Lethal Poisoning of Cancer Cells by Respiratory Chain Inhibition plus Dimethyl α-Ketoglutarate. Cell Rep 27 820 PMID: 30995479
Hart et al (2019) MARK2/Par1b kinase present at centrosomes and retraction fibres corrects spindle off-centring induced by actin disassembly. Open Biol 9 180263 PMID: 31238822
Donnelly et al (2014) HSF1 deficiency and impaired HSP90-dependent protein folding are hallmarks of aneuploid human cells. EMBO J 33 2374 PMID: 25205676
So (2014) Translational initiation regulated by ATM in dendritic cells development. Cell Death Dis 5 e1418 PMID: 25210801
Hough et al (2012) Tgf-β induced Erk phosphorylation of smad linker region regulates smad signaling. PLoS One 7 e42513 PMID: 22880011
Oberbach et al (2012) Free fatty acid palmitate impairs the vitality and function of cultured human bladder smooth muscle cells. Proc Natl Acad Sci U S A 7 e41026 PMID: 22808290
Shimbo et al (2012) Quantitative profiling of caspase-cleaved substrates reveals different drug-induced and cell-type patterns in apoptosis. Stem Cells 109 12432 PMID: 22802652
Bassett et al (2010) Epigenetic centromere specification directs aurora B accumulation but is insufficient to efficiently correct mitotic errors. Sci Rep 190 177 PMID: 20643881
Lin et al (2016) Glycogen Synthase Kinase-3β and Caspase-2 Mediate Ceramide- and Etoposide-Induced Apoptosis by Regulating the Lysosomal-Mitochondrial Axis. J Cell Sci 11 e0145460 PMID: 26727221
Estève et al (2014) Methyllysine reader plant homeodomain (PHD) finger protein 20-like 1 (PHF20L1) antagonizes DNA (cytosine-5) methyltransferase 1 (DNMT1) proteasomal degradation. J Biol Chem 289 8277 PMID: 24492612
Chou et al (2014) Mammalian target of rapamycin complex 2 modulates αβTCR processing and surface expression during thymocyte development. J Immunol 193 1162 PMID: 24981454
Duellman et al (2014) Single nucleotide polymorphism-specific regulation of matrix metalloproteinase-9 by multiple miRNAs targeting the coding exon. Nucleic Acids Res 42 5518 PMID: 24627221
Bhatnagar et al (2014) Phosphorylation and degradation of tomosyn-2 de-represses Ins secretion. J Biol Chem 289 25276 PMID: 25002582
Choubey et al (2014) BECN1 is involved in the initiation of mitophagy: it facilitates PARK2 translocation to mitochondria. Autophagy 10 1105 PMID: 24879156
Rivera-Pagán et al (2015) 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. PLoS One 10 e0125195 PMID: 25886567
Tamura et al (2015) A proteomic study of mitotic phase-specific interactors of EB1 reveals a role for SXIP-mediated protein interactions in anaphase onset. Biol Open 4 155 PMID: 25596275
Corrigan et al (2013) Automated tracking of mitotic spindle pole positions shows that LGN is required for spindle rotation but not orientation maintenance. Eur J Neurosci 12 2643 PMID: 23907121
Floyd et al (2013) Spatiotemporal organization of Aurora-B by APC/CCdh1 after mitosis coordinates cell spreading through FHOD1. J Appl Physiol (1985) 126 2845 PMID: 23613471
Briones-Orta et al (2013) Arkadia regulates tumor metastasis by modulation of the TGF-β pathway. PLoS One 73 1800 PMID: 23467611
Huang et al (2008) Calcineurin-mediated dephosphorylation of c-Jun Ser-243 is required for c-Jun protein stability and cell transformation. Oncogene 27 2422 PMID: 17952113
Sareila et al (2008) Effects of levo- and dextrosimendan on NF-kappaB-mediated transcription, iNOS expression and NO production in response to inflammatory stimuli. Br J Pharmacol 155 884 PMID: 19002103
Liang et al (2014) Regulation of YAP by mTOR and autophagy reveals a therapeutic target of tuberous sclerosis complex. Cell Cycle 211 2249 PMID: 25288394
Argadine et al (2009) The effect of denervation on protein synthesis and degradation in adult rat diaphragm muscle. J Exp Med 107 438 PMID: 19520837
Citri et al (2009) N-MthD.-aspartate receptor- and metabotropic glutamate receptor-dependent long-term depression are differentially regulated by the ubiquitin-proteasome system. Cancer Res 30 1443 PMID: 19821836
Schommer et al (2018) 27-Hydroxycholesterol increases α-synuclein protein levels through proteasomal inhibition in human dopaminergic neurons. BMC Neurosci 19 17 PMID: 29614969
Li et al (2018) Epigenetic control of IL-23 expression in keratinocytes is important for chronic skin inflammation. Nat Commun 9 1420 PMID: 29650963
Kustermann et al (2018) Loss of the novel Vcp (valosin containing protein) interactor Washc4 interferes with autophagy-mediated proteostasis in striated muscle and leads to myopathy in vivo. Autophagy 14 1911 PMID: 30010465
Lin et al (2018) Capsaicin-induced TRIB3 upregulation promotes apoptosis in cancer cells. Cancer Manag Res 10 4237 PMID: 30323679
Bouris et al (2015) Estrogen receptor alpha mediates epithelial to mesenchymal transition, expression of specific matrix effectors and functional properties of breast cancer cells. Matrix Biol 43 42 PMID: 25728938
Obakan et al (2015) SILAC-Based Mass Spectrometry Analysis Reveals That Epibrassinolide Induces Apoptosis via Activating Endoplasmic Reticulum Stress in Prostate Cancer Cells. PLoS One 10 e0135788 PMID: 26353013
Barr and Bakal (2015) A sensitised RNAi screen reveals a ch-TOG genetic interaction network required for spindle assembly. J Neurosci 5 10564 PMID: 26037491
Shrestha and Draviam (2013) Lateral to end-on conversion of chromosome-microtubule attachment requires kinesins CENP-E and MCAK. Curr Biol 23 1514 PMID: 23891108
Ren et al (2013) A critical role for protein degradation in the nucleus accumbens core in cocaine reward memory. Neuropsychopharmacology 38 778 PMID: 23303053
Luo et al (2013) Human bocavirus VP2 upregulates IFN-β pathway by inhibiting ring finger protein 125-mediated ubiquitination of retinoic acid-inducible gene-I. J Immunol 191 660 PMID: 23772026
Purnell and Fox (2013) Autophagy-mediated turnover of dynamin-related protein 1. BMC Neurosci 14 86 PMID: 23937156
Wiseman et al (2013) Proteasomal degradation of eukaryotic elongation factor-2 kinase (EF2K) is regulated by cAMP-PKA signaling and the SCFβTRCP ubiquitin E3 ligase. J Biol Chem 288 17803 PMID: 23640883
Stec et al (2013) Drosophila SOCS36E negatively regulates JAK/STAT pathway signaling via two separable mechanisms. Mol Biol Cell 24 3000 PMID: 23885117
Gouet et al (2012) On the mechanism of synaptic depression induced by CaMKIIN, an endogenous inhibitor of CaMKII. PLoS One 7 e49293 PMID: 23145145
Inácio et al (2011) Macrophage migration inhibitory factor promotes cell death and aggravates neurologic deficits after experimental stroke. J Cereb Blood Flow Metab 31 1093 PMID: 21063426
Vuolteenaho et al (2009) Leptin enhances synthesis of proinflammatory mediators in human osteoarthritic cartilage--mediator role of NO in leptin-induced PGE2, IL-6, and IL-8 production. Mediators Inflamm 2009 345838 PMID: 19688109
Kaji et al (2020) Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells Sci Rep 10 3088 PMID: 32080280
Kang (2012) Punctuated cyclin synthesis drives early embryonic cell cycle oscillations. Mol Biol Cell 23 284 PMID: 22130797
Safiulina et al (2019) Miro proteins prime mitochondria for Parkin translocation and mitophagy. EMBO J 38 PMID: 30504269
Gallego-Bartolomé et al (2019) Co-targeting RNA Polymerases IV and V Promotes Efficient De Novo DNA Methylation in Arabidopsis. Cell 176 1068 PMID: 30739798
Scrivo et al (2019) Gigaxonin E3 ligase governs ATG16L1 turnover to control autophagosome production. Nat Commun 10 780 PMID: 30770803
Han et al (2019) Post-translational regulation of lipogenesis via AMPK-dependent phosphorylation of ins.-induced gene. Nat Commun 10 623 PMID: 30733434
Padilla et al (2017) TRAF3IP2 mediates high glucose-induced endothelin-1 production as well as endothelin-1-induced inflammation in endothelial cells. Am J Physiol Heart Circ Physiol ajpheart.00478.2017 PMID: 28971844
Shrestha (2017) Aurora-B kinase pathway controls the lateral to end-on conversion of kinetochore-microtubule attachments in human cells. Nat Commun 8 150 PMID: 28751710
Feng et al (2017) Ubiquitin ligase SYVN1/HRD1 facilitates degradation of the SERPINA1 Z variant/α-1-antitrypsin Z variant via SQSTM1/p62-dependent selective autophagy. Autophagy 13 686 PMID: 28121484
McNair et al (2018) Serine protease modulation of Dependence Receptors and EMT protein expression. Cancer Biol Ther 20 349 PMID: 30403907
Zulkipli et al (2018) Spindle rotation in human cells is reliant on a MARK2-mediated equatorial spindle-centering mechanism. J Cell Biol 217 3057 PMID: 29941476
Do you know of a great paper that uses MG 132 from Tocris? Please let us know.
Reviews for MG 132
Average Rating: 5 (Based on 4 Reviews.)
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Inhibition of NF-kB activation.
By
MARINA KOUTSIOUMPA on 10/13/2022
Assay Type: In Vitro
Species: Human
MG 132 was used to block NF-kB activation and determine the pathway of a chemotherapeutic in pancreatic cancer lines. The inhibitor worked nicely, and the results were consistent
MG132.
By
Anonymous on 05/28/2021
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: H9C2
Treated H9C2 cells for 6hours to inhibit ubiquitination.
MG-132 (15 µM).
By
Anonymous on 12/11/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: LP-1 cell line
Cells were treated with MG-132 (15 µM) for 18 hours in the absence or presence of GSK2656157 (10 µM)
MG 132 Usage Information.
By
Chao Li on 01/08/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Human intestine subepithelial myofibroblasts
It works well and dissolves perfectly in DMSO. I treated the cells with MG 132 (final concentration: 10 micromolar) in serum free medium for 24 hours.
Literature in this Area
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TPD and Induced Proximity Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia