1. Metabolic Enzyme/Protease
  2. Proteasome

MG-132 

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

MG-132 is a potent, non-specific 20S proteasome inhibitor, with IC50 of 24.2 nM for the β5 chymotrypsin-like active site.

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

    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: Sci Rep. 2017 Jun 7;7(1):2929.

    Caspase signaling pathway. MCF7 and MDA-MB-231 cells are pretreated with 10 µM Z-VAD-FMK and BOC-D-FMK for 1 h and then exposed to 80 μM ω3-FFAs and 20 μM ATRA for 48 h. The expression of PARP protein.

    MG-132 purchased from MCE. Usage Cited in: Oncotarget. 2016 May 10;7(19):27176-84.

    PIG3 silencing does not affect the degradation of HIF-1α protein under hypoxia. Forty-eight hours after transfection with PIG3-siRNA or negative control siRNA, CAKI cells are pretreated under hypoxia for 4 h followed by treatment with 100 μg/mL Cycloheximide (CHX) to block protein synthesis for the indicated times. The mean values from two experiments are connected by the lines. Protein levels are analyzed by Immunoblotting, GAPDH is employed a loading control. All the experiments above are cond

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

    SR-B1 protein is degraded by proteasome pathway. (A) SR-B1 is degraded in a CHX dose-dependent manner in CHO-K1 cells. (B) Time course of SR-B1 degradation in CHO-K1 cells treated with CHX.

    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 Jul 19;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: Biochem Pharmacol. 2018 Feb 21;150:280-292.

    Expression of c-Myc in MKN-45 cells treated with Lanatoside C and SB216763 at indicated concentrations for 24 h.

    MG-132 purchased from MCE. Usage Cited in: Cell Prolif. 2018 Feb 27.

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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    MG-132 is a potent, non-specific 20S proteasome inhibitor, with IC50 of 24.2 nM for the β5 chymotrypsin-like active site.

    IC50 & Target

    IC50: 24.2 nM (chymotrypsin-like activity)[1]

    In Vitro

    Dose-dependent inhibition of cell growth is observed in HeLa cells with an IC50 of approximately 5 μM MG132 for 24 h. MG132 inhibits the growth of HeLa cells via inducing the cell cycle arrest as well as triggering apoptosis[2]. MG-132 inhibits C6 glioma cell proliferation in a time- and dose-dependent manner (the IC50 value at 24 h is 18.5 μM). MG-132 (18.5 μM) suppresses the proteasome activity by about 70% at 3 h. MG-132 induces apoptosis via down-regulation of antiapoptotic proteins Bcl-2 and XIAP, up-regulation of pro-apoptotic protein Bax and caspase-3, and production of cleaved C-terminal 85 kDa PARP. MG-132 also causes a more than 5-fold increase of reactive oxygen species[3]. The IC50 of MG-132 against HeLa, CaSki, and C33A cervical cancer cells viability after 48 h of incubation is 2.1, 3.2, and 5.2 μM, respectively[4].

    In Vivo

    The in vivo antitumor activity of MG-132 against cervical cancer is examined using s.c. xenograft models. MG-132 is injected at 1 mg/kg using the following schedule: days 1, 4, 8, 12, 15 18, 23, and 26 for mice bearing HeLa tumors. The growth inhibition rates of MG132 compared to control is 49%[4]. MG-132 (i.p., 0.1 mg/kg/day) attenuates pressure-overload-induced cardiac hypertrophy and improves cardiac function in abdominal aortic banding (AAB) rats through regulation of ERK1/2 and JNK1 signaling pathways[5].

    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Kinase Assay
    [3]

    After growing on six-well plates (3×105 cells/well) for 24 h, C6 glioma cells are treated with either PBS (control) or 18.5 μM MG-132 for 3, 6, 12, or 24 h at 37°C. Cells are thoroughly scraped from the culture dishes with a cell scraper and washed with cold PBS. After centrifugation for 10 min at 800×g, the cell pellets are suspended in ice-cold buffer (50 mM Tris-HCl, pH 7.5, 20 μM ATP, 5 mM MgCl2, 1 mM dithiothreitol, and 20% glycerol) and homogenized with a Pyrex glass microhomogenizer (20 strokes). The homogenate is centrifuged at 15 000×g for 10 min at 4°C to obtain supernatant. Protein concentration is determined using protein assay kits. A total of 10 μL (1 μg/μL) of each freshly made supernatant is incubated in a 96-well plate at 37°C for 30 min with 10 μL of 300 μM of Succinyl-LLVY-AMC and 85 μL of assay buffer (20 mM Tris-HCl, pH 7.5, and 20% glycerol). Release of fluorescent AMC is measured with a spectrofluorometer at 440 nm with an excitation wavelength of 380 nm[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    MG-132 is dissolved in PBS to a storage concentration of 50 μM[3].

    C6 glioma cells are seeded onto 96-well microplates (3×104 cells/well) and cultured for 24 h. The cells are treated with PBS or MG-132 final concentrations of 10, 20, 30, and 40 μM, respectively. Cell viability is assessed using an MTT assay at 3, 6, 12, and 24 h after MG-132 treatment. The absorbance value at 570 nm is read using an automatic multi-well spectrophotometer. C6 glioma cells (3×105 cells/well) are allowed to grow on coverslips in 6-well culture plates for 24 h. The cells are then treated with either PBS (control) or 18.5 μM MG-132 at 37°C for 24 h. Cells growing on glass coverslips are fixed in methanol for 5 min at room temperature. The fixed cells are washed twice with PBS and then incubated with Hoechst 33342 for 5 min at room temperature and observed under a fluorescence microscope. Fragmented or condensed nuclei are scored as apoptotic[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4][5]

    MG-132 is dissolved in vehicle (saline) (Mice)[4].
    MG-132 is dissolved in vehicle (0.1% DMSO) (Rats)[5].

    Mice[4]
    C.B-17/lcr-scid/scidJcl mice are inoculated s.c. with HeLa, CaSki, or C33A (1×107 cells). Tumors are allowed to grow for 1 week. Mice are killed and tumors are removed. Tumors are then cut into 2-mm diameter pieces and s.c. transplanted in C.B-17/lcr-scid/scidJcl mice (n=6 per group). One week after inoculation, mice are treated with i.v. injection of saline (control), MG-132 (1 mg/kg/dose) twice a week for 4 weeks. The volume (V) of tumors is measured before every injection, as estimated using equation V=a×b2/2 where a and b are major and minor axes of the tumor measured by a caliper, respectively.
    Rats[5]
    Male Sprague-Dawley rats (8 weeks old, 180-230 g) are used to establish pressure-overload model. All animals are separated into four groups (10 rats per group): (i) vehicle-treated sham group; (ii) MG-132-treated sham group; (iii) vehicle-treated abdominal aortic banding (AAB) group; and (iv) MG-132-treated AAB group. Under intraperitoneal pentobarbital (50 mg/kg) anesthesia, AAB is created using a 5-0 suture tied twice around the abdominal aorta in which a 21-gauge needle is inserted. The needle is then retracted yielding a 70-80% constriction with an outer aortic diameter of ~0.8 mm. In the sham surgery rats, the same surgery is performed except the aorta is constricted. At Day 3 after the surgery, MG-132-treated rats are intraperitoneally injected with 0.1 mg/kg/day of MG-132 for 8 weeks. All control animals are injected with a corresponding volume of vehicle only (0.1% DMSO). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    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

    Storage

    4°C, protect from light

    *The compound is unstable in solutions, freshly prepared is recommended.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: >98.0%

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    Product Name:
    MG-132
    Cat. No.:
    HY-13259
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