MG132

• Catalog No.: S2619
• CAS Number: 133407-82-6
• M. F.: C26H41N3O5
• M. W.: 475.62084
• Storage: -20°C

SYNONYMS

• IUPAC name: benzyl N-[(1S)-3-methyl-1-{[(1S)-3-methyl-1-{[(2S)-4-methyl-1-oxopentan-2-yl]carbamoyl}butyl]carbamoyl}butyl]carbamate
• IUPAC Traditional name: benzyl N-[(1S)-3-methyl-1-{[(1S)-3-methyl-1-{[(2S)-4-methyl-1-oxopentan-2-yl]carbamoyl}butyl]carbamoyl}butyl]carbamate
• Synonyms: MG-132

DATABASE IDS

• CAS Number: 133407-82-6

PROPERTIES

• Target: Proteasome
• Salt Data: Free Base
• Storage Condition: -20°C

DETAILS

Description (English)

Research Area

• Description: Cancer

Protocol

• Protocol: Kinase Assay ^[1]
• Measurement of inhibitory activities of MG-132 against 20S proteasome: The reaction mixture for the 20S proteasome inhibitory assay contains 0.1 M Tris-acetate, pH 7.0, 20S proteasome, MG-132, and 25 μM substrate dissolved in dimethyl sulfoxide in a final volume of 1 mL. After incuba tion at 37 °C for 15 minutes, the reaction is stopped by the addition of 0.1 mL of 10% SDS and 0.9 mL of 0.1M Tris acetate, pH 9.0. The fluorescence of the reaction products is measured. To determine the IC50 against 20S proteasome, various concentrations of MG-132 are included in the assay mixture.
• Protocol: Cell Assay ^[5]
• Cell Lines: KIM-2, HC11, and ES
• Concentrations: Dissolved in DMSO, final concentrations ~25 μM
• Incubation Time: 24, and 48 hours
• Methods: Cells are exposed to various concentrations of MG-132 for 24, and 48 hours. Supernatant and monolayer cells are harvested by centrifugation and fixed in 70% ethanol in PBS for staining with acridine orange. Equal volumes of cells and acridine orange (5 mg/mL in PBS) are mixed on a microscope slide and examined by fluorescence microscopy. For annexin V analysis, cells are harvested by centrifugation and stained with annexin V and propidium iodide. For cell cycle analysis, cells are rehydrated in PBS at room temperature for 10 minutes, followed by staining with propidium iodide (5 mg/mL). All samples are analyzed using a Coulter Epics XL flow cytometer.
• Protocol: Animal Study ^[6]
• Animal Models: Male mdx (C57BL/10ScSn DMD mdx) mice
• Formulation: Dissolved in DMSO, and diluted in PBS
• Doses: ~10 μg/kg/day
• Administration: Injection

References

• References: [1] Tsubuki S, et al. J Biochem, 1996, 119(3), 572-576.
• References: [2] Fiedler MA, et al. Am J Respir Cell Mol Biol, 1998, 19(2), 259-268.
• References: [3] Giuliano M, et al. Cancer Res, 1999, 59(21), 5586-5595.
• References: [4] Arlt A, et al. Oncogene, 2001, 20(7), 859-868.
• References: [5] MacLaren AP, et al. Cell Death Differ, 2001, 8(3), 210-218.
• References: [6] Bonuccelli G, et al. Am J Pathol, 2003, 163(4), 1663-1675.

REFERENCES

• Tsubuki S, et al. J Biochem, 1996, 119(3), 572-576.
• Fiedler MA, et al. Am J Respir Cell Mol Biol, 1998, 19(2), 259-268.
• Giuliano M, et al. Cancer Res, 1999, 59(21), 5586-5595.
• Arlt A, et al. Oncogene, 2001, 20(7), 859-868.
• MacLaren AP, et al. Cell Death Differ, 2001, 8(3), 210-218.
• Bonuccelli G, et al. Am J Pathol, 2003, 163(4), 1663-1675.