1. Metabolic Enzyme/Protease
    Autophagy
    Apoptosis
  2. Proteasome
    Autophagy
    Apoptosis
  3. MG-132

MG-132 (Synonyms: Z-Leu-leu-leu-al)

Cat. No.: HY-13259 Purity: >98.0%
Handling Instructions

MG-132 est un inhibiteur puissant et réversible du protéasome avec un IC50 de 100 nM. MG-132 bloque efficacement l'activité protéolytique du complexe de protéasome 26S. MG-132, un peptide aldéhyde, est un activateur d'autophagie.

MG-132 (Z-Leu-Leu-Leu-Al) ist ein potenter Proteasom- und Calpain-Inhibitor mit IC50-Werten von 100 nM bzw. 1,2 μM. MG-132 blockiert effektiv die proteolytische Aktivität des 26S-Proteasomkomplexes. MG-133, ein Peptidaldehyd, ist ebenfalls ein Autophagie-Aktivator.

MG-132 (Z-Leu-leu-leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.

For research use only. We do not sell to patients.

MG-132 Chemical Structure

MG-132 Chemical Structure

CAS No. : 133407-82-6

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Customer Review

Based on 169 publication(s) in Google Scholar

Other Forms of MG-132:

Top Publications Citing Use of Products

Publications Citing Use of MCE MG-132

    MG-132 purchased from MCE. Usage Cited in: Sci Rep. 2017 Jun 7;7(1):2929.

    p53 and Cell apoptosis. MCF7 and MDA-MB-231 cells are treated with 80 μM ω-3 FFAs, 20 μM ATRA alone or in combination for 48 h. The expression of PARP and p53 protein. β-Actin is used as an internal control.

    MG-132 purchased from MCE. Usage Cited in: Antioxid Redox Signal. 2019 May 20;30(15):1831-1848.

    Tan-IIA increases the endogenous induction of Nrf2 induction and this effect is further enhanced by cotreatment with the proteasome inhibitor MG-132.

    MG-132 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604.

    Different concentrations of two classical proteasome inhibitors PS-341 and MG132 are added. AGS cells are either untreated or treated with PS-341 (25 nM) or MG132 (0.1 μM) for 24 h in the absence or presence of baf A1 (100 nM).

    MG-132 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2017 Sep 2;490(4):1168-1175.

    Treatment of CHO-K1 cells with proteasome inhibitor, MG-132 results in elevated SR-B1 protein levels. The cells with MG-132, a potent proteasome inhibitor that inhibit ubiquitin/proteasome-dependent protein degradation, and MG-132 treatment significantly enhances cellular SR-B1 protein level.

    MG-132 purchased from MCE. Usage Cited in: J Inorg Biochem. 2017 Oct;175:92-100.

    TPEN-triggered PML-RARα degradation in NB4 cells is reversed by MG-132 treatment. NB4 cells are treated with 5 μM TPEN with or without the presence of 1 μM MG-132 for the indicated durations (0–12 h) and then lysed. The lysates are analyzed for PML-RARα and RARα protein levels by western blotting.

    MG-132 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Dec 1;410:112-123.

    Immunoprecipitation of ubiquitin from lysates of U-2 OS cells expressing CHOP after treatment with different concentrations of MG7 for 48 h. Cells are incubated with MG132 (20 mM) for 4 h before harvest. Cell lysates are immunoblotted with the indicated antibodies.

    MG-132 purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Feb 1;146:251-259.

    In the absence of MG132, the protein degradation pathways are intact, the Tau protein level is significantly decreased in peptide 1-treated group.

    MG-132 purchased from MCE. Usage Cited in: Cell Prolif. 2018 Aug;51(4):e12451.

    Immunoblot analysis of CDK4 in cells treated with 4 μM of CGN for 24 hours in the presence and absence of MG132.

    MG-132 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Apr 19;9:377.

    Immunoblot levels of highly molecular weight (HMW)-ubiquitinated proteins and pSer129-α-syn after inhibiting the ubiquitin-proteasome system (UPS) by various concentrations of MG132 (0.25, 0.5, and 1 μM) in SH-SY5Y cells.

    MG-132 purchased from MCE. Usage Cited in: Université de Montréal. Octobre 2017.

    Unsynchronized control and ARF6 cells are treated with DMSO or MG132 (10 μM) for 1h or 4h, lysed and total ubiquitinated proteins are determined using western blot (n=3).

    MG-132 purchased from MCE. Usage Cited in: Mol Plant Pathol. 2018 Dec;19(12):2623-2634.

    Destabilization of BRC1 mediated by SWP1 is inhibited by proteasome inhibitors Epoxomicin and MG132.

    MG-132 purchased from MCE. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Oct;1864(10):3322-3338.

    The neonatal rat cardiomyocytes (NRCMs) are treated with MG132 (10 μM). The protein expression level of PPARα in the indicated group.

    MG-132 purchased from MCE. Usage Cited in: EBioMedicine. 2018 Aug;34:243-255.

    MPC1 protein expression in primary mouse hepatocytes incubated with pyruvate for 8 h in the presence of MG-132.

    MG-132 purchased from MCE. Usage Cited in: Cancer Res. 2019 Feb 1;79(3):534-545.

    Cells are transfected with GYS2 siRNA and pre-incubated with MG-132 (20 μM) for 12 h. Cell lysate are immunoprecipitated by anti-Ub and immunoblotted by anti-p53.

    MG-132 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523.

    The accumulated poly-ubiquitinated protein is detected by Western blotting after J-Lat 10.6 cells are treated with DMSO, PR-957 (100 nM), PR-957 (150 nM) or MG132 (500 nM) for 48 h.

    MG-132 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 15;37(1):193.

    Western blot is performed in HCC-LM3 cells transfected with HJURP knockdown lentivirus and treated with DMSO or MG132.

    MG-132 purchased from MCE. Usage Cited in: Oncol Lett. 2018 Nov;16(5):5900-5906.

    Treatment with the 26S proteasome inhibitor, MG 132 (10 µM), rescues the downregulation of NEK 8 in the pVHL overexpressing SGC 7901 cells.

    MG-132 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 3;37(1):240.

    Decrease of ERCC6 expression can be rescued with proteasome inhibitor MG132. Subconfluent SKOV3 cells are treated with FL118 and MG132 alone or in combination as shown for 8 h, followed by western blot analyses with ERCC6 antibody.

    MG-132 purchased from MCE. Usage Cited in: Cell Cycle. 2018;17(13):1591-1601.

    The protein level of CCNB1 in different groups is analyzed by Western blot; MG132 significantly increases the protein level of CCNB1 in oocytes from CRS group mice. Western blotting showing the reduced expression of securin is rescued by MG132 in CRS group mouse oocytes.

    MG-132 purchased from MCE. Usage Cited in: Mol Immunol. 2018 Nov 13;104:69-78.

    Western analysis of proteins expression with treatment of IKK-16 or MG-132.

    MG-132 purchased from MCE. Usage Cited in: Molecules. 2019 Jan 22;24(3). pii: E393.

    The HepG2 cells are pretreated for 5 h MG 132 which is a proteasome inhibitor. Then, the MARCH1 protein expressions in HepG2 cells treated with 0 μM, 5,0 μM SAF, and 2.5 μM MG 132 are measured by immunoblotting.

    MG-132 purchased from MCE. Usage Cited in: Brain Behav Immun. 2019 Jul;79:244-255.

    Effect of autolysosome inhibitor (chloroquine, CQ, 50 μM) or proteasome inhibitor (MG132, 5 μM) on KA-induced NLRP3 degradation. Cells are treated with the inhibitors for 0.5 h before KA (10 μM, 2 h) treatment.

    MG-132 purchased from MCE. Usage Cited in: EMBO J. 2019 Mar 15;38(6):e100376.

    Brcc3+/+ and Brcc3-/- (Abro1+/+ and Abro1-/-)BMDMs are treated with or without LPS for 1 h. Before LPS treatment, Brcc3-/- (Abro1-/-) BMDMs are pretreated with MG132 (10 μM) for 6 h to rescue the expression of ABRO1. Immunoblot analysis of NLRP3 and ABRO1 proteins in cell lysates immunoprecipitated with anti-ABRO1 antibody.

    MG-132 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 26;38(1):101.

    HLF and Hep3B cells are treated with Mg132 (10 μg/ml) for 4 h, total protein is extracted and subjected to western blotting using anti-Flag, anti-p21, or anti-GAPDH antibodies.

    MG-132 purchased from MCE. Usage Cited in: J Exp Bot. 2019 Sep 24;70(18):4749-4762.

    Cell-free degradation assay of recombinant His-PhCHS protein. Recombinant His- PhCHS is purified from Escherichia coli incubated with petal crude proteins at stages and treated with specific 26S proteasome inhibitor MG132 at various time intervals. Western blot analysis was conducted using an anti-His antibody and anti-β-actin protein concentration was used as a loading control.

    MG-132 purchased from MCE. Usage Cited in: Cell Rep. 2020 Aug 4;32(5):107990.

    PMs are treated with MG132 (10 μM). Endogenous YAP protein accumulated in the presence of MG132 starts from 2 h and further increases at 4 and 6 h after treatment in WT macrophages.
    • Biological Activity

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    • References

    • Customer Review

    Description

    MG-132 (Z-Leu-leu-leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator[1][2][3]. MG-132 also induces apoptosis[2].

    IC50 & Target

    IC50: 100 nM (Proteasome), 1.2 μM (Calpain)[1][3]

    In Vitro

    MG-132 initiates neurite outgrowth in PC12 cells at a low concentration (30 nM) and is a very strong inhibitor of 20S proteasome[3].
    MG-132 (10 μM; 1 hour) reverses the effects of TNF- α on I κ B degradation and NF-κ B activation in A549 cells[4].
    MG-132 (0.75-5 μM; 24 hours) potently induces p53-dependent apoptosis in KIM-2 cells by 26S proteasome inhibition[5].
    MG-132 (10-40 μM; 24 hours) significantly reduces the viability of C6 glioma cells in both time- and concentration-dependent manners and shows the IC50 of 18.5 μM at 24 hours[6].
    MG-132 (18.5 μM; 24 hours) induces down-regulation of anti-apoptotic proteins Bcl-2 and XIAP and up-regulates expression of pro-apoptotic protein Bax and caspase-3[6].

    Cell Viability Assay[3]

    Cell Line: C6 glioma cells
    Concentration: 10, 20, 30, 40 μM
    Incubation Time: 24 hours
    Result: Significantly reduced the viability of C6 glioma cells beginning at 6 h in both time- and concentration-dependent manners and showed the IC50 of 18.5 μM at 24 hours.

    Western Blot Analysis[3]

    Cell Line: A549 cells
    Concentration: 10 μM
    Incubation Time: 1 hour
    Result: Reversed the effects of TNF-α on IκB degradation and resulted in a reversal of TNF-α-induced NF-κB activation.
    In Vivo

    MG132 (10 mg/kg; i.p.; daily for 25 days starting 5 days after EC9706 cells injection) significantly inhibits tumor growth of the EC9706 xenograft without causing toxicity to mice[7].
    MG-132 (1 mg/kg; i.v.; twice a week for 4 weeks) shows potent tumor inhibitory effect against mice bearing HeLa tumors[8].
    MG-132 (1-10 μg/kg/24 hours; subcutaneously implanted osmotic pumps; for 8 days) greatly increases the expression levels of β-dystroglycan, α-dystroglycan, α-sarcoglycan, and dystrophin in skeletal muscle lysates in mice (six-month-old male C57BL/10ScSn DMD mdx mice)[9].

    Animal Model: 5- to 6-weeks old female athymic nude mice (EC9706 xenograft)
    Dosage: 10 mg/kg
    Administration: I.p.; daily for 25 days starting 5 days after EC9706 cells injection
    Result: Significantly inhibited tumor growth of the EC9706 xenograft without causing toxicity to the mice.
    Animal Model: Five-week-old female C.B-17/lcr-scid/scidJcl mice (bearing HeLa cells)[8]
    Dosage: 1 mg/kg
    Administration: Intravenous injection; twice a week for 4 weeks
    Result: The growth inhibition rates in HeLa tumors was 49% compared to the control.
    Molecular Weight

    475.62

    Formula

    C₂₆H₄₁N₃O₅

    CAS No.

    133407-82-6

    SMILES

    O=C(OCC1=CC=CC=C1)N[[email protected]](C(N[[email protected]@H](CC(C)C)C(N[[email protected]](C([H])=O)CC(C)C)=O)=O)CC(C)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 83.33 mg/mL (175.20 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1025 mL 10.5126 mL 21.0252 mL
    5 mM 0.4205 mL 2.1025 mL 4.2050 mL
    10 mM 0.2103 mL 1.0513 mL 2.1025 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.37 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.37 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: >98.0%

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    Keywords:

    MG-132Z-Leu-leu-leu-alMG132MG 132ProteasomeAutophagyApoptosispeptidealdehydeproteolytic26SproteasomecomplexcalpainInhibitorinhibitorinhibit

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    Cat. No.:
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