IF 28
PMID: 40883572 ↗MG-132
Catalog No.: GC10383Purity:>98.00%Synonyms: ZLeuLeuLeuCHO
MG-132 is a potent proteasome and calpain inhibitor with IC50 values of 100nM and 1.25μM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 133407-82-6
10mM (in 1mL DMSO)In Stock
$26.00
1
1mgIn Stock
$11.00
1
5mgIn Stock
$25.00
1
10mgIn Stock
$33.00
1
25mgIn Stock
$70.00
1
50mgIn Stock
$109.00
1
100mgIn Stock
$167.00
1
200mgIn Stock
$234.00
1
500mgIn Stock
$386.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $26.00 | In Stock | 1 | |
| 1mg | $11.00 | In Stock | 1 | |
| 5mg | $25.00 | In Stock | 1 | |
| 10mg | $33.00 | In Stock | 1 | |
| 25mg | $70.00 | In Stock | 1 | |
| 50mg | $109.00 | In Stock | 1 | |
| 100mg | $167.00 | In Stock | 1 | |
| 200mg | $234.00 | In Stock | 1 | |
| 500mg | $386.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citations
40 publicationsPublications from researchers using this productDescription
MG-132 is a potent proteasome and calpain inhibitor with IC50 values of 100nM and 1.25μM, respectively[1]. MG-132 can cause upregulation of Nrf2-dependent antioxidative function and downregulation of NF-κB-mediated inflammation[2]. MG-132 has been widely used to alleviate the progression of arthritis and pain in rats[3].
In vitro, MG-132 treatment for 24 hours significantly inhibited the proliferation of C6 cells, with an IC50 value of 18.5μM[4]. Treatment with 1μM MG-132 for 24 hours significantly induced apoptosis in U87MG cells and A172 cells, accompanied by an increase in mitochondrial membrane potential and nuclear translocation of mitochondrial protein AIF[5]. Treatment with 1μM MG-132 for 24 hours significantly inhibited DNA synthesis in SW1116 and HT-29 cells and activated the BMP signaling pathway, resulting in cell growth inhibition[6].
In vivo, MG-132 treatment via intraperitoneal injection at a dose of 10μg/kg/day for 7 days significantly improved the cardiac function of the mouse model of myocarditis induced by Coxsackievirus B3 and inhibited the structural remodeling of the ventricle[7]. A single intraperitoneal injection of MG-132 at a dose of 9mg/kg for 6 hours significantly mitigated the liver swelling, degeneration and inflammatory cell infiltration in the acute liver injury mouse model[8].
References:
[1] Tsubuki S, Saito Y, Tomioka M, et al. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine[J]. The journal of biochemistry, 1996, 119(3): 572-576.
[2] Wang Y, Sun W, Du B, et al. Therapeutic effect of MG-132 on diabetic cardiomyopathy is associated with its suppression of proteasomal activities: roles of Nrf2 and NF-κB[J]. American Journal of Physiology-Heart and Circulatory Physiology, 2013, 304(4): H567-H578.
[3] Ahmed A S, Ahmed M, Li J, et al. Proteasome inhibitor MG 132 modulates inflammatory pain by central mechanisms in adjuvant arthritis[J]. International journal of rheumatic diseases, 2017, 20(1): 25-32.
[4] Fan W, Hou Y, Meng F, et al. Proteasome inhibitor MG-132 induces C6 glioma cell apoptosis via oxidative stress[J]. Acta Pharmacologica Sinica, 2011, 32(5): 619-625.
[5] Ko J K, Choi C H, Kim Y K, et al. The proteasome inhibitor MG-132 induces AIF nuclear translocation through down-regulation of ERK and Akt/mTOR pathway[J]. Neurochemical research, 2011, 36(5): 722-731.
[6] Wu W K K, Sung J J Y, Wu Y C, et al. Bone morphogenetic protein signalling is required for the anti‐mitogenic effect of the proteasome inhibitor MG‐132 on colon cancer cells[J]. British journal of pharmacology, 2008, 154(3): 632-638.
[7] Zhang X M, Li Y C, Chen P, et al. MG-132 attenuates cardiac deterioration of viral myocarditis via AMPK pathway[J]. Biomedicine & Pharmacotherapy, 2020, 126: 110091.
[8] Shan C, Ou D, Xiong Y, et al. Molecular mechanism of anti-inflammatory effects of the proteasome inhibitor MG-132 on Con A-induced acute liver injury in mice[J]. Research in Veterinary Science, 2023, 156: 60-65.
Protocol
| Cell experiment [1]: | |
|
Cell lines |
C6 cells |
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Preparation Method |
C6 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum (FBS), 2mM glutamine and 1% penicillin-streptomycin at 37°C in 5% CO2/atmosphere. C6 cells cultured were seeded onto 96-well microplates (3×104 cells/well) and cultured for 24h. The cells were treated with PBS or MG-132 at final concentrations of 10, 20, 30, and 40µM, respectively. After 24h incubation, cell viability was assessed. |
|
Reaction Conditions |
10, 20, 30, and 40µM; 24h |
|
Applications |
MG-132 treatment reduced the cell viability of C6 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Female athymic nude mice |
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Preparation Method |
Female athymic nude mice (6-weeks old) were housed under controlled temperature (21-23°C), humidity (30-35%) and light cycle (7:00 AM to 7:00 PM) and maintained on a standard rodent diet. Mice were inoculated intraperitoneally (i.p.) with 7×106 EC9706 cells, after which mice received injections with vehicle or MG-132 (10mg/kg/day; i.p.) for 25 days starting 5 days after the injection of EC9706 cells. Mice were fed with antioxidant-free AIN-76A special diet for a week before starting the experiment. Analyze the tumor volume of the mice every five days. |
|
Dosage form |
10mg/kg/day; 25 days; i.p. |
|
Applications |
MG-132 treatment significantly inhibited tumor growth in the EC9706 xenograft mouse model. |
References: [1] Fan W, Hou Y, Meng F, et al. Proteasome inhibitor MG-132 induces C6 glioma cell apoptosis via oxidative stress[J]. Acta Pharmacologica Sinica, 2011, 32(5): 619-625. [2] Dang L, Wen F, Yang Y, et al. Proteasome inhibitor MG132 inhibits the proliferation and promotes the cisplatin-induced apoptosis of human esophageal squamous cell carcinoma cells[J]. International journal of molecular medicine, 2014, 33(5): 1083-1088. | |
Product Documents
Purity:>98.00%Appearance:A solid
Biological Data
1 / 6
Chemical Properties
CAS No.
133407-82-6
Synonyms
ZLeuLeuLeuCHO
Chemical Name
benzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
SMILES
CC(C)CC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
Molecular Formula
C26H41N3O5
Molecular Weight
475.6
Solubility
≥ 23.78mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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