MG-132

Catalog No.: A11043
Proteasome inhibitor
MG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM).
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5mg
$20.00
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10mg
$30.00
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25mg
$55.00
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50mg
$95.00
In stock
100mg
$155.00
In stock
200mg
$280.00
In stock
500mg
$490.00
In stock
10mM * 1mL in DMSO
$30.00
In stock
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Important Notice: For research use only. We do not sell to patients.

Adooq Products cited in reputable paper
Adooq's MG-132 has been cited by 16 publications
  • Laurence J Seabrook, .et al. , Nat Chem Biol, 2024, Dec;20(12):1566-1576 PMID: 39414979
  • Nathan Bulangalire, .et al. , Biochimie, 2024, Apr 16:S0300-9084(24)00079-8 PMID: 38636798
  • Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
  • Carolina N Franco, .et al. , Sci Adv, 2023, Sep 8;9(36):eadi2232 PMID: 37682999
  • Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
  • Vo Thi Anh Nguyet, .et al. , Biochim Biophys Acta Gen Subj, 2022, Sep 6;1866(12):130241 PMID: 36075516
  • Jalila Chagraoui, .et al. , Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
  • Eunsu Yoo, .et al. , BMC Cancer, 2020, Sep 14;20(1):881 PMID: 32928152
  • Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
  • Chi-Hung R Or, .et al. , Int J Mol Sci, 2020, Mar 5;21(5):1773 PMID: 32150830
  • Ghosh S, .et al. , Biochemistry, 2020, Feb 18;59(6):780-789 PMID: 31977203
  • Kondo H, .et al. , J Biol Chem, 2020, Feb 7;295(6):1658-1672 PMID: 31915251
  • Ohigashi I, .et al. , Cell Rep, 2019, Nov 26;29(9):2901-2916 PMID: 31775054
  • Paudel DB, .et al. , Virology, 2018, Nov;524:127-139 PMID: 30195250
  • Ohkusu-Tsukada K, .et al. , Int Arch Allergy Immunol, 2018, 176(2):91-100 PMID: 29669333
  • Chi-Hung R. Or, .et al. , Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
  • Biological Activity
    Discription MG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM).
    Targets
    Target Value
    Cell Research
    Cell Line Type Value Description References
    In Vitro
    • Proteasome inhibition:
      MG-132 is a highly potent proteasome inhibitor, showing over 1000-fold greater activity than ZLLal in inhibiting the ZLLL-MCA-degrading activity of the 20S proteasome, with an IC50 of 100 nM compared to 110 μM. This potency extends to other proteasome-mediated processes, such as protein degradation and signaling regulation【1】.

    • Calpain inhibition:
      In addition to proteasome inhibition, MG-132 also inhibits calpain with an IC50 of 1.2 μM, indicating its dual capability in targeting both proteasomal and calpain-mediated pathways【1】.

    • Induction of neurite outgrowth:
      MG-132 promotes neurite outgrowth in PC12 cells at an optimal concentration of 20 nM, demonstrating approximately 500 times higher potency compared to ZLLal. This highlights its potential applications in neuroregenerative research【1】.

    • Suppression of NF-κB activation:
      At 10 μM, MG-132 effectively blocks TNF-α-induced NF-κB activation in A549 cells by preventing proteasome-mediated degradation of IκBα. This also leads to significant inhibition of interleukin-8 (IL-8) gene transcription and protein release, showcasing its anti-inflammatory properties【2】.

    • p53-dependent apoptosis induction:
      MG-132 induces p53-dependent apoptosis in KIM-2 cells through the inhibition of the 26S proteasome, emphasizing its role in triggering apoptosis in cancer cells【3】.

    • Selective apoptotic activity in multiple myeloma:
      MG-132 exhibits distinct apoptotic effects on multiple myeloma cells (U266 and OPM-2), demonstrating higher sensitivity compared to other proteasome inhibitors like BzLLLCOCHO or PS-341. However, it shows relatively weaker inhibition of the chymotrypsin-like (CT-L) and peptidylglutamyl peptide hydrolyzing (PGPH) activities of the 26S proteasome【4】.

    • Sensitization of resistant cancer cells:
      At 1 μM, MG-132 sensitizes TRAIL-resistant prostate cancer cells by activating AP-1 transcription factors such as c-Fos and c-Jun, which suppress the anti-apoptotic protein c-FLIP(L), leading to enhanced apoptosis【5】.

    • Synergistic effects with other agents:
      MG-132 significantly enhances the anti-cancer effects of inositol hexakisphosphate (IP6) in androgen-independent prostate cancer cell lines (PC3 and DU145) by reducing cellular metabolic activity. This demonstrates its potential for combination therapies in resistant cancer types【6】.

    References
    1. Tsubuki S, et al. J Biochem, 1996, 119(3), 572-576. PMID: 8647096
    2. Fiedler MA, et al. Am J Respir Cell Mol Biol, 1998, 19(2), 259-268. PMID: 9698634
    3. MacLaren AP, et al. Cell Death Differ, 2001, 8(3), 210-218. PMID: 11313715
    4. Crawford LJ, et al. Cancer Res, 2006, 66(12), 6379-6386. PMID: 16778200
    5. Li W, et al. Cancer Res, 2007, 67(5), 2247-2255. PMID: 17332343
    6. Diallo JS, et al. Br J Cancer, 2008, 99(10), 1613-1622. PMID: 18941434
    7. Bonuccelli G, et al. Am J Pathol, 2003, 163(4), 1663-1675. PMID: 14507663
    8. Caron AZ, et al. BMC Musculoskelet Disord, 2011, 12:185. PMID: 21835004
    9. Mroczkiewicz M, et al. J Med Chem, 2010, 53(4), 1509-18. PMID: 20148550
    Product Information
    Catalog Num A11043
    Formula C26H41N3O5
    Molecular Weight 475.6
    CAS Number 133407-82-6
    SMILES CC(C)C[C@@H](C=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)OCC1=CC=CC=C1
    Synonyms Z-Leu-Leu-Leu-CHO, Z-LLL-CHO, MG132
    Storage

    Store lyophilized at -20ºC, keep desiccated.
    In lyophilized form, the chemical is stable for 36 months.
    In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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