Catalog Number: 1748
Alternate Names: Z-LLL-al, Z-Leu-Leu-Leu-CHO
Chemical Name: N-[(Phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide
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
  • Solubility:
    Soluble to 100 mM in ethanol and to 100 mM in DMSO
  • Purity:
    >95%
  • Storage:
    Store at -20°C
  • CAS No:
    133407-82-6
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.
Background References
  1. Potential of the proteasome inhibitor MG-132 as an anticancer agent, alone and in combination.
    Banerjee and Liefshitz
    Anticancer Res., 2001;21:3941
  2. The ubiquitin-proteasome pathway is required for processing the NF-κB1 precursor protein and the activation of NF-κB.
    Palombella et al.
    Cell, 1994;78:773
  3. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-Leucine and tri-Leucine.
    Tsubuki et al.
    J.Biochem., 1996;119:572
Citations:

The citations listed below are publications that use Tocris products. Selected citations for MG 132 include:

34 Citations: Showing 1 - 10
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  1. Aurora-B kinase pathway controls the lateral to end-on conversion of kinetochore-microtubule attachments in human cells.
    Authors: Shrestha
    Nat Commun 2017;8(1):150
  2. 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
  3. A sensitised RNAi screen reveals a ch-TOG genetic interaction network required for spindle assembly.
    Authors: Barr and Bakal
    J Neurosci 2015;5:10564
  4. 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
  5. Extracellular glutamate exposure facilitates group I mGluR-mediated epileptogenesis in the hippocampus.
    Authors: Zhao Et al.
    Respir Res 2015;35:308
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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
  11. Phosphorylation and degradation of tomosyn-2 de-represses insulin secretion.
    Authors: Bhatnagar Et al.
    J Biol Chem 2014;289:25276
  12. Regulation of YAP by mTOR and autophagy reveals a therapeutic target of tuberous sclerosis complex.
    Authors: Liang Et al.
    Cell Cycle 2014;211:2249
  13. Mammalian target of rapamycin complex 2 modulates αβTCR processing and surface expression during thymocyte development.
    Authors: Chou Et al.
    J Immunol 2014;193:1162
  14. BECN1 is involved in the initiation of mitophagy: it facilitates PARK2 translocation to mitochondria.
    Authors: Choubey Et al.
    Autophagy 2014;10:1105
  15. Arkadia regulates tumor metastasis by modulation of the TGF-β pathway.
    Authors: Briones-Orta Et al.
    PLoS One 2013;73:1800
  16. A critical role for protein degradation in the nucleus accumbens core in cocaine reward memory.
    Authors: Ren Et al.
    Neuropsychopharmacology 2013;38:778
  17. 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
  18. Drosophila SOCS36E negatively regulates JAK/STAT pathway signaling via two separable mechanisms.
    Authors: Stec Et al.
    Mol Biol Cell 2013;24:3000
  19. Lateral to end-on conversion of chromosome-microtubule attachment requires kinesins CENP-E and MCAK.
    Authors: Shrestha and Draviam
    Curr Biol 2013;23:1514
  20. 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
  21. Autophagy-mediated turnover of dynamin-related protein 1.
    Authors: Purnell and Fox
    BMC Neurosci 2013;14:86
  22. 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
  23. 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
  24. Molecular mechanism of mutant p53 stabilization: the role of HSP70 and MDM2.
    Authors: Wiech Et al.
    PLoS One 2012;7:e51426
  25. Tgf-β induced Erk phosphorylation of smad linker region regulates smad signaling.
    Authors: Hough Et al.
    PLoS One 2012;7:e42513
  26. 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
  27. 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
  28. 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
  29. Epigenetic centromere specification directs aurora B accumulation but is insufficient to efficiently correct mitotic errors.
    Authors: Bassett Et al.
    Sci Rep 2010;190:177
  30. N-methyl-D-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
  31. 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
  32. The effect of denervation on protein synthesis and degradation in adult rat diaphragm muscle.
    Authors: Argadine Et al.
    J Exp Med 2009;107:438
  33. Calcineurin-mediated dephosphorylation of c-Jun Ser-243 is required for c-Jun protein stability and cell transformation.
    Authors: Huang Et al.
    Oncogene 2008;27:2422
  34. 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
Expand to show all 34 Citations

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