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MG-132

Key inhibitor for use in proteasome research.
 
BML-PI102-0005 5 mg 55.00 USD
 
BML-PI102-0025 25 mg 184.00 USD
Do you need bulk/larger quantities?
 
Replaces Prod. #: ALX-260-092

  • High purity peptide
  • Most economical MG-132 on the market
  • Widely cited for more than two decades
  • Well-characterized with a variety of applications
MG-132 is a potent, cell permeable and selective proteasome inhibitor (Ki = 4nM).1 It inhibits NF-κB activation by preventing IκB degradation (IC50 = 3μM). The peptide blocks degradation of short-lived proteins, which in turn induces HSP and ER chaperone expression, leading to thermotolerance (1μM MG-132, 2 h.). It also stimulates neurite outgrowth in PC12 cells (20nM optimal). The peptide has also been reported to increase the survival rate of mesenchymal stem cells following their transplantation. IC50’s for inhibition of Suc-LLVY-AMC and Z-LLL-AMC cleaving activities of proteasome were 0.85 and 0.1μM respectively. The ubiquitin-proteasome system (UPS) and autophagy serve as two complementary, reciprocally regulated protein degradation systems, thus blockade of UPS by MG-132 activates autophagy.

Product Specification

Alternative Name:Z-LLL-CHO
 
Sequence:Z-Leu-Leu-Leu-CHO
 
Formula:C26H41N3O5
 
MW:475.6
 
CAS:133407-82-6
 
Purity:≥98%
 
Appearance:White solid.
 
Solubility:Soluble in DMSO (25mg/ml) or 100% ethanol (25mg/ml).
 
Shipping:Shipped on Dry Ice
 
Long Term Storage:-80°C
 
Use/Stability:Solutions are stable for up to one week if stored at -20°C. Solutions are stable for up to two months if stored at -80°C.
 
Technical Info/Product Notes: Replacement for ADI-HPK-116
 
BML-PI102 structure
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BML-PI102 structure

Product Literature References

Intrinsic ubiquitin E3 ligase activity of histone acetyltransferase Hbo1 for estrogen receptor α: M. Iizuka, et al.; Proc. Jpn. Acad. Ser. B Phys. Biol. Sci. 93, 498 (2017), Abstract; Full Text
WIP promotes in-vitro invasion ability, anchorage independent growth and EMT progression of A549 lung adenocarcinoma cells by regulating RhoA levels: A. Salvi, et al.; Biochem. Biophys. Res. Commun. 482, 1353 (2017), Abstract;
Adjustments of Protein Metabolism in Fasting Arctic Charr, Salvelinus alpinus: A.A. Cassidy, et al.; PLoS One 11, e0153364 (2016), Application(s): 20S proteasome activity, Abstract; Full Text
Agonist-Mediated Activation of STING Induces Apoptosis in Malignant B Cells: C.A. Tang, et al.; Cancer Res. 76, 2137 (2016), Application(s): Stimulated cells, Abstract; Full Text
Copper diethyldithiocarbamate as an activator of Nrf2 in cultured vascular endothelial cells: T. Fujie, et al.; J. Biol. Inorg. Chem. 21, 263 (2016), Application(s): Cell culture, Abstract; Full Text
Cytotoxicity and Proteasome Inhibition by Alkaloid Extract from Murraya koenigii Leaves in Breast Cancer Cells-Molecular Docking Studies: A. Ismail, et al.; J. Med. Food. 12, 1155 (2016), Abstract;
Glycan-binding F-box protein from Arabidopsis thaliana protects plants from Pseudomonas syringae infection: K. Stefanowicz, et al.; BMC Plant Biol. 16, 213 (2016), Application(s): Hormone treatments, abiotic stress applications and infection assays on WT A. thaliana plants, Abstract; Full Text
HECT-Type Ubiquitin E3 Ligase ITCH Interacts With Thioredoxin-Interacting Protein and Ameliorates Reactive Oxygen Species-Induced Cardiotoxicity: Y. Otaki, et al.; J. Am. Heart Assoc. 5, e002485 (2016), Application(s): Incubated into rat cardiomyocytes, Abstract; Full Text
Inhibition of β-catenin signaling by phenobarbital in hepatoma cells in vitro: N. Groll, et al.; Toxicology 370, 94 (2016), Application(s): Cell culture, mouse hepatoma cells , Abstract;
LRRK2 interferes with aggresome formation for autophagic clearance: Y. Bang, et al.; Moll. Cell Neurosci. 75, 71 (2016), Application(s): Induced protein quality control-associated autophagy in mice to uncover how the autophagy pathway is affected, Abstract;
Mifepristone increases mRNA translation rate, triggers the unfolded protein response, increases autophagic flux, and kills ovarian cancer cells in combination with proteasome or lysosome inhibitors: L. Zhang, et al.; Mol. Oncol. 10, 1099 (2016), Application(s): In vitro exposure of the cells to drugs, Abstract;
Phosphorylation of CHIP at Ser20 by Cdk5 promotes tAIF-mediated neuronal death: C. Kim, et al.; Cell Death Differ. 23, 333 (2016), Application(s): Cell Culture, Abstract;
PIAS3 enhances the transcriptional activity of HIF-1α by increasing its protein stability: K. Nakagawa, et al. ; Biochem. Biophys. Res. Commun. 469, 470 (2016), Application(s): Immunoprecipitation and Western blotting, Abstract;
Posttranscriptional control of NLRP3 inflammasome activation in colonic macrophages: A.A. Filardy, et al.; Mucosal Immunol. 9, 850 (2016), Application(s): Cell culture, Abstract;
Proteasomal degradation of sphingosine kinase 1 and inhibition of dihydroceramide desaturase by the sphingosine kinase inhibitors, SKi or ABC294640, induces growth arrest in androgen-independent LNCaP-AI prostate cancer cells: M. McNaughton, et al.; Oncotarget 7, 16663 (2016), Application(s): Cell culture, Abstract; Full Text
A point mutation in the ubiquitin ligase RNF170 that causes autosomal dominant sensory ataxia destabilizes the protein and impairs inositol 1,4,5-trisphosphate receptor-mediated Ca2+ signaling: F.A. Wright, et al.; J. Biol. Chem. 290, 13948 (2015), Application(s): Cell Culture, Abstract; Full Text
ADAM12 and ADAM17 are essential molecules for hypoxia-induced impairment of neural vascular barrier function: D. Cui, et al.; Sci. Rep. 5, 12796 (2015), Application(s): Cell Culture, Abstract;
Cinnamic aldehyde suppresses hypoxia-induced angiogenesis via inhibition of hypoxia-inducible factor-1α expression during tumor progression: W.Y. Bae, et al.; Biochem. Pharmacol. 98, 41 (2015), Application(s): Cell culture , Abstract;
D1 dopamine receptor stimulation impairs striatal proteasome activity in Parkinsonism through 26S proteasome disassembly: P. Barroso-Chinea, et al.; Neurobiol. Dis. 78, 77 (2015), Application(s): Assay, Abstract;
Fatty acids increase adiponectin secretion through both classical and exosome pathways: V. DeClercq, et al.; Biochim. Biophys. Acta 1851, 1123 (2015), Application(s): Cell Culture, Abstract;
Molecular Consequences of Defective SERPINH1/HSP47 in the Dachshund Natural Model of Osteogenesis Imperfecta: U. Lindert, et al.; J. Biol. Chem. 290, 17679 (2015), Application(s): Cell Culture, Western Blot, Abstract; Full Text
NEDD8 Ultimate Buster-1 Long (NUB1L) Protein Suppresses Atypical Neddylation and Promotes Proteasomal Degradation of Misfolded Proteins: J. Li, et al.; J. Biol. Chem. 290, 23850 (2015), Application(s): Proteasomal peptidase activity assay, Abstract; Full Text
RGS19 Converts Iron Deprivation Stress into a Growth-Inhibitory Signal: J. Hwang, et al.; Biochem. Biophys. Res. Commun. 464, 168 (2015), Application(s): Cell Culture, Abstract;
Signal transduction and downregulation of C-MET in HGF stimulated low and highly metastatic human osteosarcoma cells: K. Husmann, et al.; Biochem. Biophys. Res. Commun. 464, 1222 (2015), Application(s): Cell Culture, Abstract;
UBXN2A regulates nicotinic receptor degradation by modulating the E3 ligase activity of CHIP: Y. Teng, et al.; Biochem. Pharmacol. 97, 518 (2015), Application(s): Cell culture, Abstract;
Variable Processing and Cross-presentation of HIV by Dendritic Cells and Macrophages Shapes CTL Immunodominance and Immune Escape: J. Dinter, et al.; PLoS Pathog. 11, e1004725 (2015), Application(s): Cell Culture, Abstract; Full Text
Identification and characterization of RING-finger ubiquitin ligase UBR7 in mammalian spermatozoa: S. Zimmerman, et al.; Cell Tissue Res. 356, 261 (2014), Application(s): IF, WB of boar, mouse and human sperm , Abstract;
Kizuna is a novel mitotic substrate for CDC25B phosphatase: Y. Thomas, et al.; Cell Cycle 13, 3867 (2014), Application(s): HeLa, U2OS, and U2OS Tet-off cells analyzed by IP, IF , Abstract; Full Text
Pivotal role for ROS activation of p38 MAPK in the control of differentiation and tumor-initiating capacity of glioma-initiating cells: A. Sato, et al.; Stem Cell Res. 12, 119 (2014), Application(s): WB of human glioma-initiating cells, Abstract;
The small heat shock protein B8 (HSPB8) confers resistance to bortezomib by promoting autophagic removal of misfolded proteins in multiple myeloma cells: M. Hamouda, et al.; Oncotarget 5, 6252 (2014), Application(s): Analysis of velcade resistant multiple myeloma human cells by WB, Assay, Abstract; Full Text
A20 restricts wnt signaling in intestinal epithelial cells and suppresses colon carcinogenesis: L. Shao, et al.; PLoS One 8, e62223 (2013), Application(s): IF, WB of mouse intestinal epithelial cells , Abstract; Full Text
Pathogen signatures activate a ubiquitination pathway that modulates the function of the metabolic checkpoint kinase mTOR: S. Ivanov & C. Roy; Nat. Immunol. 14, 1219 (2013), Application(s): Analysis of mouse macrophages by WB, PCR, Abstract; Full Text
The ubiquitin proteasome system regulates the stability and activity of the glucose sensor glucokinase in pancreatic beta cells: A. Hofmeister-Brix, et al.; Biochem. J. 456, 173 (2013), Abstract; Full Text
Autophagy plays a protective role in endoplasmic reticulum stress-mediated pancreatic β cell death: A. Bartolome, et al.; Autophagy 8, 1757 (2012), Application(s): Flow cytometry of fetal pancreatic β cells , Abstract; Full Text
Enhanced protein repair and recycling are not correlated with longevity in 15 vertebrate endotherm species: K.D. Salway, et al.; Age 33, 33 (2011), Abstract;
Novel Cell- and Tissue-Based Assays for Detecting Misfolded and Aggregated Protein Accumulation Within Aggresomes and Inclusion Bodies: D. Shen, et al.; Cell Biochem. Biophys. 60, 173 (2011), Abstract; Full Text
SUMO E3 ligase activity of TRIM proteins: Y. Chu & X. Yang; Oncogene 30, 1108 (2011), Application(s): Mammalian in vitro cells analyzed by WB, Abstract; Full Text
Induction of autophagy by proteasome inhibitor is associated with proliferative arrest in colon cancer cells: W.K. Wu, et al.; BBRC 374, 258 (2008), Abstract;
Role of proteasomal degradation in the cell cycle-dependent regulation of DNA topoisomerase IIalpha expression: L. Salmena, et al.; Biochem. Pharmacol. 61, 795 (2001), Abstract;
Proteasome inhibitors activate stress kinases and induce Hsp72. Diverse effects on apoptosis: A.B. Meriin, et al.; J. Biol. Chem. 273, 6373 (1998), Abstract;
Proteasome inhibition leads to a heat-shock response, induction of endoplasmic reticulum chaperones, and thermotolerance: K.T. Bush, et al.; J. Biol. Chem. 272, 9086 (1997), Abstract;
J. Adams & R. Stein; Ann. Rep. Med. Chem. 31, 279 (1996),
Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine: S. Tsubuki, et al.; J. Biochem. 119, 572 (1996), Abstract;
Selective inhibitors of the proteasome-dependent and vacuolar pathways of protein degradation in Saccharomyces cerevisiae: D.H. Lee & A.L. Goldberg; J. Biol. Chem. 271, 27280 (1996), Abstract;
The human cytomegalovirus US11 gene product dislocates MHC class I heavy chains from the endoplasmic reticulum to the cytosol: E.J. Wiertz, et al.; Cell 84, 769 (1996), Abstract;
Multiple proteolytic systems, including the proteasome, contribute to CFTR processing: T.J. Jensen, et al.; Cell 83, 129 (1995), Abstract;
The proteasome pathway is required for cytokine-induced endothelial-leukocyte adhesion molecule expression: M.A. Read, et al.; Immunity 2, 493 (1995), Abstract;
Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules: K.L. Rock, et al.; Cell 78, 761 (1994), Abstract;

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