MG 132

Catalog # Availability Size / Price Qty
MG 132 | CAS No. 133407-82-6 | Calpain Inhibitors
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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%

Product Details
Citations (60)

Biological Activity

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

Soluble to 100 mM in ethanol and to 100 mM in DMSO
Store at -20°C

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.

Background References

  1. Tgf-beta induced Erk phosphorylation of smad linker region regulates smad signaling.
    Hough C, Radu M, Dore J
    PLoS ONE, 2012;7(8):e42513.
  2. Delayed Recovery of Skeletal Muscle Mass following Hindlimb Immobilization in mTOR Heterozygous Mice.
    Lang SM, Kazi AA, Hong-Brown L, Lang CH
    PLoS ONE, 2012;7(6):e38910.
  3. Rhinovirus 3C protease suppresses apoptosis and triggers caspase-independent cell death
    M Lötzerich, PS Roulin, K Boucke, R Witte, O Georgiev, UF Greber
    Cell Death Dis, 2018;9(3):272.
  4. Ubiquitin-specific protease 25 functions in Endoplasmic Reticulum-associated degradation.
    Blount JR, Burr AA, Denuc A
    PLoS ONE, 2012;7(5):e36542.
  5. Glucocorticoids mediate induction of microRNA-708 to suppress ovarian cancer metastasis through targeting Rap1B.
    Lin, Kai-Ti, Yeh, Yu-Ming, Chuang, Chi-Mu, Yang, Scarlett, Chang, Jer-Wei, Sun, Shu-Pin, Wang, Yi-Shian, Chao, Kuan-Cho, Wang, Lu-Hai
    Nat Commun, 2015;6(0):5917.
  6. MicroRNAs located in the Hox gene clusters are implicated in huntington's disease pathogenesis.
    Hoss, Andrew G, Kartha, Vinay K, Dong, Xianjun, Latourelle, Jeanne C, Dumitriu, Alexandr, Hadzi, Tiffany, Macdonald, Marcy E, Gusella, James F, Akbarian, Schahram, Chen, Jiang-Fa, Weng, Zhiping, Myers, Richard
    PLoS Genet, 2014;10(2):e1004188.
  7. Reversible modification of adenomatous polyposis coli (APC) with K63-linked polyubiquitin regulates the assembly and activity of the beta-catenin destruction complex.
    Tran H, Polakis P
    J Biol Chem, 2012;287(34):28552-63.
  8. Proteasome proteolysis supports stimulated platelet function and thrombosis.
    Gupta N, Li W, Willard B, Silverstein R, McIntyre T
    Arterioscler Thromb Vasc Biol, 2014;34(1):160-8.
  9. Resolvin D1 Improves the Resolution of Inflammation via Activating NF-?B p50/p50-Mediated Cyclooxygenase-2 Expression in Acute Respiratory Distress Syndrome
    Y Gao, H Zhang, L Luo, J Lin, D Li, S Zheng, H Huang, S Yan, J Yang, Y Hao, H Li, F Gao Smith, S Jin
    J. Immunol., 2017;0(0):.
  10. Truncation of the TAR DNA-binding protein 43 is not a prerequisite for cytoplasmic relocalization, and is suppressed by caspase inhibition and by introduction of the A90V sequence variant
    HJ Wobst, L Delsing, NJ Brandon, SJ Moss
    PLoS ONE, 2017;12(5):e0177181.
  11. Expression of constitutively active CDK1 stabilizes APC-Cdh1 substrates and potentiates premature spindle assembly and checkpoint function in G1 cells.
    Ma Y, Yuan X, Wyatt WR
    PLoS ONE, 2012;7(3):e33835.
  12. Sequential actions of the AAA-ATPase valosin-containing protein (VCP)/p97 and the proteasome 19 S regulatory particle in sterol-accelerated, endoplasmic reticulum (ER)-associated degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase.
    Morris L, Hartman I, Jun D, Seemann J, Debose-Boyd R
    J Biol Chem, 2014;289(27):19053-66.
  13. Potential of the proteasome inhibitor MG-132 as an anticancer agent, alone and in combination.
    Banerjee and Liefshitz
    Anticancer Res., 2001;21:3941
  14. 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
  15. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-Leucine and tri-Leucine.
    Tsubuki et al.
    J.Biochem., 1996;119:572
  16. 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;
  17. Intracellular trafficking of adeno-associated virus vectors: routing to the late endosomal compartment and proteasome degradation
    Douar et al.
    J.Virol., 2001;75:1824

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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

  1. 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
  2. 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
  3. Miro proteins prime mitochondria for Parkin translocation and mitophagy.
    Authors: Safiulina Et al.
    EMBO J  2019;38
  4. Lethal Poisoning of Cancer Cells by Respiratory Chain Inhibition plus Dimethyl α-Ketoglutarate.
    Authors: Sica Et al.
    Cell Rep  2019;27:820
  5. Co-targeting RNA Polymerases IV and V Promotes Efficient De Novo DNA Methylation in Arabidopsis.
    Authors: Gallego-Bartolomé Et al.
    Cell  2019;176:1068
  6. Gigaxonin E3 ligase governs ATG16L1 turnover to control autophagosome production.
    Authors: Scrivo Et al.
    Nat Commun  2019;10:780
  7. Post-translational regulation of lipogenesis via AMPK-dependent phosphorylation of ins.-induced gene.
    Authors: Han Et al.
    Nat Commun  2019;10:623
  8. Epigenetic control of IL-23 expression in keratinocytes is important for chronic skin inflammation.
    Authors: Li Et al.
    Nat Commun  2018;9:1420
  9. 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
  10. Serine protease modulation of Dependence Receptors and EMT protein expression.
    Authors: McNair Et al.
    Cancer Biol Ther  2018;20:349
  11. 27-Hydroxycholesterol increases α-synuclein protein levels through proteasomal inhibition in human dopaminergic neurons.
    Authors: Schommer Et al.
    BMC Neurosci  2018;19:17
  12. 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.
    Autophagy  2018;14:1911
  13. Capsaicin-induced TRIB3 upregulation promotes apoptosis in cancer cells.
    Authors: Lin Et al.
    Cancer Manag Res  2018;10:4237
  14. 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
  15. 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
  16. 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.
    Autophagy  2017;13:686
  17. Noncanonical SQSTM1/p62-Nrf2 pathway activation mediates proteasome inhibitor resistance in multiple myeloma cells via redox, metabolic and translational reprogramming.
    Authors: Riz Et al.
    Oncotarget  2016;7:66360
  18. 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.
    Oncotarget  2016;7:13984
  19. Atrogin-1 Deficiency Leads to Myopathy and Heart Failure in Zebrafish.
    Authors: Bühler Et al.
    Int J Mol Sci  2016;17
  20. 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
  21. A sensitised RNAi screen reveals a ch-TOG genetic interaction network required for spindle assembly.
    Authors: Barr and Bakal
    J Neurosci  2015;5:10564
  22. 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
  23. 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
  24. Extracellular glutamate exposure facilitates group I mGluR-mediated epileptogenesis in the hippocampus.
    Authors: Zhao Et al.
    Respir Res  2015;35:308
  25. 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
  26. 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
  27. 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
  28. 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
  29. Translational initiation regulated by ATM in dendritic cells development.
    Authors: So
    Cell Death Dis  2014;5:e1418
  30. 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
  31. HSF1 deficiency and impaired HSP90-dependent protein folding are hallmarks of aneuploid human cells.
    Authors: Donnelly Et al.
    EMBO J  2014;33:2374
  32. 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
  33. Phosphorylation and degradation of tomosyn-2 de-represses Ins secretion.
    Authors: Bhatnagar Et al.
    J Biol Chem  2014;289:25276
  34. Regulation of YAP by mTOR and autophagy reveals a therapeutic target of tuberous sclerosis complex.
    Authors: Liang Et al.
    Cell Cycle  2014;211:2249
  35. Mammalian target of rapamycin complex 2 modulates αβTCR processing and surface expression during thymocyte development.
    Authors: Chou Et al.
    J Immunol  2014;193:1162
  36. 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
  37. BECN1 is involved in the initiation of mitophagy: it facilitates PARK2 translocation to mitochondria.
    Authors: Choubey Et al.
    Autophagy  2014;10:1105
  38. Arkadia regulates tumor metastasis by modulation of the TGF-β pathway.
    Authors: Briones-Orta Et al.
    PLoS One  2013;73:1800
  39. A critical role for protein degradation in the nucleus accumbens core in cocaine reward memory.
    Authors: Ren Et al.
    Neuropsychopharmacology  2013;38:778
  40. 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
  41. Drosophila SOCS36E negatively regulates JAK/STAT pathway signaling via two separable mechanisms.
    Authors: Stec Et al.
    Mol Biol Cell  2013;24:3000
  42. Lateral to end-on conversion of chromosome-microtubule attachment requires kinesins CENP-E and MCAK.
    Authors: Shrestha and Draviam
    Curr Biol  2013;23:1514
  43. 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
  44. Autophagy-mediated turnover of dynamin-related protein 1.
    Authors: Purnell and Fox
    BMC Neurosci  2013;14:86
  45. 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
  46. 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
  47. Molecular mechanism of mutant p53 stabilization: the role of HSP70 and MDM2.
    Authors: Wiech Et al.
    PLoS One  2012;7:e51426
  48. On the mechanism of synaptic depression induced by CaMKIIN, an endogenous inhibitor of CaMKII.
    Authors: Gouet Et al.
    PLoS One  2012;7:e49293
  49. Tgf-β induced Erk phosphorylation of smad linker region regulates smad signaling.
    Authors: Hough Et al.
    PLoS One  2012;7:e42513
  50. 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
  51. 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
  52. Punctuated cyclin synthesis drives early embryonic cell cycle oscillations.
    Authors: Kang
    Mol Biol Cell  2012;23:284
  53. 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
  54. 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
  55. Epigenetic centromere specification directs aurora B accumulation but is insufficient to efficiently correct mitotic errors.
    Authors: Bassett Et al.
    Sci Rep  2010;190:177
  56. 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
  57. 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
  58. The effect of denervation on protein synthesis and degradation in adult rat diaphragm muscle.
    Authors: Argadine Et al.
    J Exp Med  2009;107:438
  59. 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
  60. 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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