Free shipping on all orders over $ 500

MG132

Cat. No. M1902
MG132 Structure
Size Price Availability Quantity
10mg USD 75 In stock
50mg USD 220 In stock
100mg USD 300 In stock
Bulk Inquiry?

Quality Control
Biological Activity

MG132 is a potent cell-permeable inhibitor of proteasome and calpain with IC50 of 100 nM and 1.2 μM respectively. Proteasome inhibitors are emerging as a new class of anticancer agents. MG132 inhibited the growth of HeLa cells via inducing the cell cycle arrest as well as triggering apoptosis. MG132 also inhibits NF-κB activation with an IC50 of 3 µM and prevents β-secretase cleavage. MG132 induces cell apoptosis through formation of reactive oxygen species or the upregulation and downregulation of these factors, which is ultimately dependent upon the activation of the caspase family of cysteine proteases. In vitro, it induces neurite outgrowth in PC12 cells and has anticancer properties. Besides its apoptotic effect alone, MG132 also enhanced the antiglioma effect of the chemotherapeutics cisplatin, taxol and doxorubicin in C6 and U138MG cells, indicating an adjuvant/chemosensitizer potential.

Protocol
Cell Experiment
Cell lines Lung cancer cell lines A549 and H1299
Preparation method Cell viability assay. Cell viability was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells were seeded in 96-well plates at a density of 2.5x103/well 1 day prior to treatment. Then, cells were treated with MG132 or/and irradiation. After treatment, 20 µl of 5 mg/ml MTT solution was added into each well and incubated for 4 h. After the supernatant was removed, 100 µl of DMSO was added, and then placed in a microplate reader to measure OD value. Cell viability rate (vR) was calculated according to the following formula: vR = (OD in observed group/OD in 0 Gy group) x 100%. All assays were repeated 3 times in quintuplicate.
Concentrations 200 nM
Incubation time 6h
Animal Experiment
Animal models H1299 cells Xenograft tumorigenicity in nude mice
Formulation saline
Dosages unknown
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 475.63
Formula C26H41N3O5
CAS Number 133407-82-6
Purity 100.00%
Solubility DMSO 90 mg/mL
Ethanol 90 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Journal of Hematology & Oncology (2017). Figure 5. MG132 (Abmole Bioscience)
Method Immunofluorescence analysis
Cell Lines U251, U87 and U118 cell lines
Concentrations 20 μM
Incubation Time 2 h
Results Astrocytoma patients with a low expression of SIX3 and mutant p53 are more sensitive to treatment with aurora kinase inhibitors.
Rating
Source Journal of Hematology & Oncology (2017). Figure 3. MG132 (Abmole Bioscience)
Method Western blotting
Cell Lines U251, U87 and U118 cell lines
Concentrations 20 μM
Incubation Time 2 h
Results When we knocked down AURKA, MG132 resulted in increased AURKB expression and had less effect on AURKA (Fig. 3e).
Rating
Source Institut für Biochemie der Universität Stuttgart (2014). Figure 21. MG132 (Abmole Bioscience)
Method MG-132 was dissolved in DMSO. To verify that the activity was sufficiently inhibited, peptide cleavage assays were performed.
Cell Lines
Concentrations 200 μM
Incubation Time 2 h
Results As shown above, GST-Nup53 was immobilized on glutathione sepharose beads (Figure 21A, load, bottom lane; Coomassie blue stained gel) and incubated with equal amounts of CP or Blm10-CP. To confirm that equal amounts of proteasome were used, the loads were separated by SDS-PAGE, and the gel was subsequently stained with Coomassie blue and immunoblotted against the HA-tag of 4 (Figure 21A, load).
Rating
Source Faculté de Médecine (2015). Figure 5. MG132 (Abmole Bioscience, Kowloon, Honk Hong)
Method
Cell Lines CFBE-wt cells
Concentrations 5 μM
Incubation Time 18h
Results In fact, our data obtained in the presence of MG132 and/or cycloheximide (Fig. 4 and 5) indicated that CFTR synthesis may also be affected by PsaDM. Our study, as well as data from the literature, thus indicated that P. aeruginosa exoproducts may impact CFTR protein synthesis, degradation and trafficking/recycling to the cell membrane.
Rating
Source Faculté de Médecine (2015). Figure 4. MG132 (Abmole Bioscience, Kowloon, Honk Hong)
Method
Cell Lines CFBE-wt cells
Concentrations 5 μM
Incubation Time 18h
Results In fact, our data obtained in the presence of MG132 and/or cycloheximide (Fig. 4 and 5) indicated that CFTR synthesis may also be affected by PsaDM. Our study, as well as data from the literature, thus indicated that P. aeruginosa exoproducts may impact CFTR protein synthesis, degradation and trafficking/recycling to the cell membrane.
Rating
Source ERJ Express.(2015). Figure 5. MG132 (Abmole Bioscience, Kowloon, Honk Hong)
Method Immunoblotting
Cell Lines CFBE-ΔF508 and CFBE-wt cell lines
Concentrations
Incubation Time 18 h
Results To confirm that the huge accumulation of CFTR protein observed after proteasomal inhibition with MG132 (MG132+LB at 18 h) (fig. 5a and b) was secondary to newly synthesised CFTR proteins, we verified that a co treatment with CHX (MG132+CHX+LB) totally prevented CFTR accumulation.
Rating
Source ERJ Express.(2015). Figure 4. MG132 (Abmole Bioscience, Kowloon, Honk Hong)
Method Immunoblotting
Cell Lines CFBE-ΔF508 and CFBE-wt cell lines
Concentrations
Incubation Time 2 h, 8 h, 18 h
Results In fact, our data obtained in the presence of MG132 and/or CHX (figs 4 and 5) indicated that CFTR synthesis may also be affected by PsaDM.
Rating
Source Autophage (2016) . Figure 2. MG132 (Abmole BioScience, M1902)
Method Western blot
Cell Lines HEK293T, MCF7 or MDA-MB-231 cells
Concentrations 10 μM
Incubation Time 6 h
Results Results showed that NH4Cl, but not MG132, 3-MA or wortmannin, induced the accumulation of HSD17B4 protein (Fig. 2A ), indicating that the degradation of HSD17B4 is independent of the proteasome and macroautophagy pathways.
Rating
Product Citations
References

MG132, a proteasome inhibitor, induces apoptosis in tumor cells.
Guo N, et al. Asia Pac J Clin Oncol. 2012 May 15. PMID: 22897979.

Proteasome inhibitor MG132 induces selective apoptosis in glioblastoma cells through inhibition of PI3K/Akt and NFkappaB pathways, mitochondrial dysfunction, and activation of p38-JNK1/2 signaling.
Zanotto-Filho A, et al. Invest New Drugs. 2012 Feb 28. PMID: 22367315.

The effect of MG132, a proteasome inhibitor on HeLa cells in relation to cell growth, reactive oxygen species and GSH.
Han YH, et al. Oncol Rep. 2009 Jul;22(1):215-21. PMID: 19513526.

Related Proteasome Products
Sivelestat sodium tetrahydrate

Sivelestat sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse.

MG-101

MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM). IC50 value: 150 nM (Ki)

VR23

VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM).

Gabexate Mesylate

Gabexate Mesylate is a serine protease inhibitor with IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation.

CEP-18770

CEP-18770 is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MG132 supplier, Proteasome, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.