MG-132 (Synonyms: ZLeuLeuLeuCHO) |
Catalog No.GC10383
One-Click Copy Product Info
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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
Sample solution is provided at 25 µL, 10mM.
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- bioRxiv (2024):2024-02.
- eGastroenterology 2.1 (2024).
- bioRxiv (2024):2024-10.
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.
| Cell experiment [1]: | |
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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. |
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Reaction Conditions |
10, 20, 30, and 40µM; 24h |
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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. |
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Dosage form |
10mg/kg/day; 25 days; i.p. |
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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. | |
| Cas No. | 133407-82-6 | SDF | |
| 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 | ||
| Canonical SMILES | CC(C)CC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1 | ||
| Formula | C26H41N3O5 | M.Wt | 475.6 |
| Solubility | ≥ 23.78mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1026 mL | 10.513 mL | 21.0261 mL |
| 5 mM | 420.5 μL | 2.1026 mL | 4.2052 mL |
| 10 mM | 210.3 μL | 1.0513 mL | 2.1026 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
Clarification of FBW7 as the E3 ubiquitin ligase of cPLA2 protein. (C) DLD1WT cell was treated with 50μM MG132 for 6h and then blotted with cPLA2 antibody.
DLD1WT cell was treated with MG132(50μM, for 6h) (GlpBio, USA).
Cell Reports Medicine (2024). PMID: 38614093 IF: 14.2994 -
Related Biological Data
Silent information regulator 2 (SIRT2) increased glucose 6-phosphate dehydrogenase. A, B, G6PD protein expression levels were analyzed by western blot analysis in stably transfected ACHN and Caki-1 cells following treatment with 100 μg/mL cycloheximide (CHX) with or without 10 μg/mL MG132 for 0, 6, 9, 12h.
Proteasome inhibitor MG132 (#GC10383; GLPBIO) powder was dissolved in DMSO to prepare 10 mg/mL storage solution.
Cancer Science (2021). PMID: 34310804 IF: 6.712 -
Related Biological Data
Depletion of TgATG7 results in TgATG8 degradation through ubiquitin-proteasome system. (G) HA-TgATG8 was co-expressed along with either FLAG-UbWT or FLAG-UbKO and its stability was monitored in the presence or absence of CHX and MG132 using anti-HA antibody.
The stability of endogenous TgATG8 protein was tested with or without the addition of CHX (10 μg/ml) and MG132 (15μM) (GlpBio, USA).
Bba-Mol Basis Dis (2023): 166891. PMID: 37739091 IF: 6.2001 -
Related Biological Data
DHA reduces DNMT1 and enhances Klotho levels. h Representative Western blot analyses of DNMT1 expression are shown in primary mouse renal tubular cells(PRTCs).
Primary mouse renal tubular cells(PRTCs) were treated with TGF-β (10ng/mL) and DHA (10μM) in combination with MG132(0.5µM)(GlpBio, USA), E64d (10µg/mL), or ammonium chloride (NHCl; 1mM) for 24 h.
Acta Pharmacologica Sinica (2022): 1-15. PMID: 35347248 IF: 6.1496 -
Related Biological Data
PHLDA1 regulates YWHAE levels through proteasomal degradation pathways. (A, B) Western blot analysis of YWHAE expression; cells were treated with MG132 alone or MG132+6% CSE.
Moreover, the reduction of YWHAE level caused by CSE or PHLDA1 siRNA could be rescued by MG132(GlpBio, USA), a proteasome inhibitor.
Int J Biochem Cell B (2022): 106297. PMID: 36108948 IF: 5.6521 -
Related Biological Data
Increased apoptosis induced by VRK1 depletion is driven by DNA-PK instability. (E) OVCAR-4 cells were treated with 2μM of VRK1 inhibitor. After 24 h, the cells were treated with MG132 (50μg/ml) for 6h. After treatment, cells were harvested and subjected to DNA-PK IP and ubiquitination was analyzed using western blotting.
Cells were treated with 50μg/ml MG132 (cat. no. GC10383, GLPBIO, CA, USA) for 6h.
Experimental Cell Research (2024): 114036. PMID: 38614421 IF: 3.7001
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