(R)-MG132 |
| Catalog No.GC41233 |
(R)-MG132 is a proteasome inhibitor with an IC50 of 100 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1211877-36-9
Sample solution is provided at 25 µL, 10mM.
(R)-MG132 is a proteasome inhibitor with an IC50 of 100 nM. This compound of (R)-MG132 and IC50 effectively inhibits the proteolytic function of the 26S proteasome complex, leading to induced autophagy and apoptosis. Moreover, (R)-MG132 exhibits notable efficacy in inhibiting tumor growth[1-2].
(R)-MG132(10- 40 μM ; 3-24h) suppressed the proliferation of C6 glioma cells and also inhibited the chymotrypsin-like activity of the proteasome[3]. (R)-MG132(1 μM;24h) triggers the nuclear translocation of AIF by down-regulating the ERK and Akt/mTOR pathways[4]. The combination of GSK-470 and (R)-MG132 (200 nM; 24 hours) leads to nearly complete inhibition of AKT activity and mTORC1/mTORC2 activity[5].
(R)-MG132(10μg/kg; i.p; daily for 7 days) regulated the AMPK signaling pathway, thereby modulating apoptosis and inflammation, enhancing hemodynamics, and inhibiting ventricular structural remodeling in a myocarditis mouse model [6]. Treatment with (R)-MG132(0.1mg/kg; i.p) significantly mitigated cancer cachexia, as evidenced by reduced weight loss, altered carbohydrate metabolism, decreased muscle atrophy, increased spontaneous activity, and extended survival time in tumor-bearing mice[7].
References:
[1]. Harhouri K, Navarro C, et.al. MG132-induced progerin clearance is mediated by autophagy activation and splicing regulation. EMBO Mol Med. 2017 Sep;9(9):1294-1313. doi: 10.15252/emmm.201607315. PMID: 28674081; PMCID: PMC5582415.
[2]. Tsubuki S, Saito Y, , et.al. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. J Biochem. 1996 Mar;119(3):572-6. doi: 10.1093/oxfordjournals.jbchem.a021280. PMID: 8830056.
[3]. Fan WH, Hou Y, , et.al. Proteasome inhibitor MG-132 induces C6 glioma cell apoptosis via oxidative stress. Acta Pharmacol Sin. 2011 May;32(5):619-25. doi: 10.1038/aps.2011.16. Epub 2011 Apr 18. PMID: 21499287; PMCID: PMC4002511.
[4]. Ko JK, Choi CH, , et.al. The proteasome inhibitor MG-132 induces AIF nuclear translocation through down-regulation of ERK and Akt/mTOR pathway. Neurochem Res. 2011 May;36(5):722-31. doi: 10.1007/s11064-010-0387-9. Epub 2011 Jan 4. PMID: 21203833.
[5]. Zhang J, Yang C, , et.al. PDK1 inhibitor GSK2334470 synergizes with proteasome inhibitor MG‑132 in multiple myeloma cells by inhibiting full AKT activity and increasing nuclear accumulation of the PTEN protein. Oncol Rep. 2018 Jun;39(6):2951-2959. doi: 10.3892/or.2018.6369. Epub 2018 Apr 12. PMID: 29658600.
[6]. Zhang XM, Li YC, et.al. MG-132 attenuates cardiac deterioration of viral myocarditis via AMPK pathway. Biomed Pharmacother. 2020 Jun;126:110091. doi: 10.1016/j.biopha.2020.110091. Epub 2020 Apr 8. PMID: 32278272.
[7]. Zhang L, Tang H, et.al. MG132-mediated inhibition of the ubiquitin-proteasome pathway ameliorates cancer cachexia. J Cancer Res Clin Oncol. 2013 Jul;139(7):1105-15. doi: 10.1007/s00432-013-1412-6. Epub 2013 Mar 28. PMID: 23535871; PMCID: PMC7087863.
| Cell experiment [1]: | |
Cell lines | Rat C6 glioma cells |
Preparation Method | Cells were seeded onto 96-well microplates and cultured for 24 hours. Subsequently, the cells were treated with (R)-MG132 at final concentrations ranging from 10 to 40 μM for durations of 3 to 24 hours. |
Reaction Conditions | 10-μM ; 3-24h |
Applications | (R)-MG132 inhibited the proliferation of C6 glioma cells in a time- and dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male BALB/c mice (CVB3 cell induced acute viral myocarditis models) |
Preparation Method | Mice were administered (R)-MG132 intraperitoneally on a daily basis starting the day after CVB3 inoculation. |
Dosage form | 10μg/kg; i.p; daily for 7days |
Applications | (R)-MG132 demonstrates anti-apoptotic and anti-inflammatory properties in the context of myocardial injuries induced by CVB3. |
References: [1]:Fan WH, Hou Y,et,al. Proteasome inhibitor MG-132 induces C6 glioma cell apoptosis via oxidative stress. Acta Pharmacol Sin. 2011 May;32(5):619-25. doi: 10.1038/aps.2011.16. Epub 2011 Apr 18. PMID: 21499287; PMCID: PMC4002511. [2]:Zhang XM, Li YC, et,al. MG-132 attenuates cardiac deterioration of viral myocarditis via AMPK pathway. Biomed Pharmacother. 2020 Jun;126:110091. doi: 10.1016/j.biopha.2020.110091. Epub 2020 Apr 8. PMID: 32278272. | |
| Cas No. | 1211877-36-9 | SDF | |
| Canonical SMILES | O=CC[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)OCc1ccccc1 | ||
| Formula | C26H41N3O5 | M.Wt | 475.6 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 25 mg/ml | 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 | 0.4205 mL | 2.1026 mL | 4.2052 mL |
| 10 mM | 0.2103 mL | 1.0513 mL | 2.1026 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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 ddH2O, 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Related Biological Data
Penetration efficiency of peptide KKP.(E) Fluorescence intensity quantification of FITC-labeled KKP1 (7.5 μM) treated with different time points (with or without the MG132 treatment) corresponding to the fluorescence microscopy shown in(D).
(R)-MG132 (GC41233) was obtained from GLPBIO (Montclair,CA, USA).
Acs Pharmacol Transl 6.1 (2022): 76-87. PMID: 36654751 IF: 5.9998 -
Related Biological Data
HNK increases protein ubiquitination by inhibiting proteasome activity. e NB4 cells were treated with HNK (0 or 30 μM) for 24 h, and the cells were collected for 20S protease activity determination. 1 μM (R)-MG-132 was used as a positive control.
In the presence or absence of (R)-MG-132(1 μM)(GLPBIO), the same amount of 30 μg protein, 20 μM fluorescent substrate (Suc-Leu-Leu-Val-Tyr-AMC) and a proper amount of buffer were distributed into a black 96-well plate with transparent substrate.
Apoptosis (2021): 1-14. PMID: 33550458 IF: 4.67
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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