MG-132(R)

Alias: R-isomer of MG-132; MG132; MG 132; (R)-MG 132; (R)-MG-132; (R)-MG132
Cat No.:V0559 Purity: ≥98%
MG-132 (R) (R-isomer of MG-132),a peptide aldehyde, is a novel, potent, non-specific, cell permeable and reversible inhibitor 20S proteasome inhibitor, with IC50of 24.2 nM for the β5 chymotrypsin-like active site.
MG-132(R) Chemical Structure CAS No.: 1211877-36-9
Product category: Proteasome
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
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Other Forms of MG-132(R):

  • MG-132
Official Supplier of:
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Top Publications Citing lnvivochem Products
InvivoChem's MG-132(R) has been cited by 2 publications
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

MG-132 (R) (R-isomer of MG-132), a peptide aldehyde, is a novel, potent, non-specific, cell permeable and reversible inhibitor 20S proteasome inhibitor, with IC50 of 24.2 nM for the β5 chymotrypsin-like active site. In lysates of J558L multiple myeloma cells and EMT6 breast cancer cells, it can inhibit proteasome activity. For chymotrypsin-like (ChTL), trypsin-like (TL), and peptidylglutamyl peptide hydrolyzing proteasome (PGPH) activities, the (R)-MG132 stereoisomer is a more potent inhibitor than (S)-MG132.

Biological Activity I Assay Protocols (From Reference)
Targets
Proteasome
ln Vitro
(R)-MG-132, the stereoisomer of MG-132, is being investigated as a possible inhibitor of the proteasome's ability to hydrolyze peptidylglutamyl peptide, trypsin, and chymotrypsin-like activities[1]. The effects of MG-132 and (R)-MG-132 on the inhibition of trypsin-like (TL), peptidylglutamyl peptide hydrolyzing (PGPH), and ChTL of purified 20S proteasomes isolated from human erythrocytes are being studied. MG-132 has IC₅₀ values of 0.89 μM, 104.43 μM, and 5.7 μM for ChTL, TL, and PGPH, in that order. The IC₅₀ values for ChTL, TL, and PGPH of (R)-MG-132 are 0.22 μM, 34.4 μM, and 2.95 μM, respectively[1].
ln Vivo
In skeletal muscle fibers from mdx mice, MG-132 administration efficiently restores the expression levels and plasma membrane localization of dystrophin, β-dystroglycan, α-bdystroglycan, and α-sarcoglycan, minimizes damage to muscle membranes, and improves the histopathological symptoms of muscular dystrophy.[8] By downregulating the muscle-specific ubiquitin ligases atrogin-1/MAFbx and MuRF-1 mRNA, MG-132 treatment dramatically reduces immobilization-induced skeletal muscle atrophy in mice.[8]
Enzyme Assay
MG-132, 20S proteasome, pH 7.0, 0.1 M Tris-acetate, and 25 μM substrate dissolved in dimethyl sulfoxide in a final volume of 1 mL make up the reaction mixture for the 20S proteasome inhibitory assay. 0.1 mL of 10% SDS and 0.9 mL of 0.1M Tris acetate, pH 9.0, are added to stop the reaction after it has been incubated at 37 °C for 15 minutes. The reaction products' fluorescence is measured. Different concentrations of MG-132 are added to the assay mixture in order to calculate the IC50 against 20S proteasome.
Cell Assay
MG-132 is added to cells at different concentrations for 24, and 48 hours. Centrifugation is used to collect the supernatant and monolayer cells, which are then preserved in 70% ethanol in PBS before being stained with acridine orange. Acridine orange (5 mg/mL in PBS) and equal volumes of cells are combined on a microscope slide, and fluorescence microscopy is used to examine the mixture. Cells are collected by centrifugation and stained with propidium iodide and annexin V for annexin V analysis. Propidium iodide (5 mg/mL) staining is done after rehydrating cells in PBS at room temperature for ten minutes in order to analyze the cell cycle. Utilizing a Coulter Epics XL flow cytometer, every sample is examined.
Animal Protocol
Male mdx (C57BL/10ScSn DMD mdx) mice
~10 μg/kg/day
Injection
References

[1]. J Biochem . 1996 Mar;119(3):572-6.

[2]. Am J Respir Cell Mol Biol . 1998 Aug;19(2):259-68.

[3]. Cell Death Differ . 2001 Mar;8(3):210-8.

[4]. Cancer Res . 2006 Jun 15;66(12):6379-86.

[5]. J Med ChemCancer Res . 2007 Mar 1;67(5):2247-55.

[6]. Br J Cancer . 2008 Nov 18;99(10):1613-22.

[7]. Am J Pathol . 2003 Oct;163(4):1663-75.

[8]. BMC Musculoskelet Disord . 2011 Aug 15:12:185.

[9]. J Med Chem . 2010 Feb 25;53(4):1509-18.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H41N3O5
Molecular Weight
475.62
Exact Mass
475.30
Elemental Analysis
C, 65.66; H, 8.69; N, 8.83; O, 16.82
CAS #
1211877-36-9
Appearance
Solid powder
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
InChi Key
TZYWCYJVHRLUCT-ZRBLBEILSA-N
InChi Code
InChI=1S/C26H41N3O5/c1-17(2)12-21(15-30)27-24(31)22(13-18(3)4)28-25(32)23(14-19(5)6)29-26(33)34-16-20-10-8-7-9-11-20/h7-11,15,17-19,21-23H,12-14,16H2,1-6H3,(H,27,31)(H,28,32)(H,29,33)/t21-,22+,23-/m0/s1
Chemical Name
benzyl N-[(2S)-4-methyl-1-[[(2R)-4-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
Synonyms
R-isomer of MG-132; MG132; MG 132; (R)-MG 132; (R)-MG-132; (R)-MG132
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~95 mg/mL (~199.7 mM)
Water: <1 mg/mL
Ethanol: ~95 mg/mL (~199.7 mM)
Solubility (In Vivo)
4% DMSO+30% PEG 300+20% propylene glycol+ddH2O: 2 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • MG-132(R)

  • MG-132(R)

  • MG-132(R)

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