MG 132

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Cat.No. 1748 - MG 132 | C26H41N3O5 | CAS No. 133407-82-6
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)
Datasheet
Citations (33)
Literature

Biological Activity

Potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM). Inhibits TNF-α-induced NF-κB activation and IκBα degradation. Induces neurite outgrowth in PC12 cells and has anticancer properties in vitro.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 47.56 100
ethanol 47.56 100

Preparing Stock Solutions

The following data is based on the product molecular weight 475.63. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


If you know of a relevant reference for MG 132, please let us know.

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View all Proteasome Inhibitors

Keywords: 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 Z-LLL-al Z-Leu-Leu-Leu-CHO Proteasome

33 Citations for MG 132

Citations are publications that use Tocris products. Selected citations for MG 132 include:

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

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

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-methyl-D-aspartate receptor- and metabotropic glutamate receptor-dependent long-term depression are differentially regulated by the ubiquitin-proteasome system. Cancer Res 30 1443 PMID: 19821836

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

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

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

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

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

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 insulin 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

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

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

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

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


Do you know of a great paper that uses MG 132 from Tocris? If so please let us know.

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