MG-262 (Synonyms: PS-III,MG262,MG 262) |
| Catalog No.GC15517 |
A proteasome inhibitor with diverse biological activities
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 179324-22-2
Sample solution is provided at 25 µL, 10mM.
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MG-262 (also known as Z-Leu-Leu-Leu-B(OH)2), a boronic peptide acid, is a potent proteasome inhibitor that selectively and reversibly inhibits the chymotryptic activity of the proteasome. It consists of a peptide and boronic acid moiety which are functional to proteasome inhibition. According to previous studies, MG-262 is capable of reducing the viability of nasal mucosa and polyp fibroblasts, provoking cell growth arrest, inhibiting DNA replication and retinoblastoma phosphorylation, increasing expression of the cell cycle inhibitor p21 and p27, and inducing cell death via loss of mitochondrial membrane potential, caspase-3 and poly(ADP-ribose) polymerase activation, induction of c-Jun phosphorylation and mitogen-activated protein kinase phosphatase-1 expression.
Reference
[1].Laura Pujols, Laura Fernandez-Bertolin, Mireya Fuentes-Prado, Isam Alobid, Jordi Roca-Ferrer, Neus Agell, Joaquim Mullol, and Cesar Picado. Proteasome inhibition reduces proliferation, collagen expression, and inflammatory cytokine production in nasal mucosa and polyp fibroblasts. The Journal of Pharmacology and Experimental Therapeutics 2012; 343:184-197
[2].Hilary Frase, Jason Hudak, and Irene Lee. Identification of the proteasome inhibitor MG262 as a potent ATP-dependent inhibitor of the Salmonella enteric serovar typhimurium lon protease. Biochemistry 2006; 45 (27): 8264-8274
| Cell experiment: [1] | |
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Cell lines |
Peripheral blood mononuclear cells (PBMC) |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
0.01 μM, 28 days |
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Applications |
TRAP positive and multi-nucleated osteoclasts were quantified by light microscopy after 28 days of MG-262 treatment. The used proteasome inhibitor was sufficient for significant inhibition of osteoclast formation, while the effects occurred in a dose-dependent manner. The differentiation was reduced to 27% for 0.01 μM and to 30% for 0.001 μM. |
| Animal experiment: [2] | |
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Animal models |
GFPdgn TG mice |
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Dosage form |
Intravenous injection, 5 μmol/kg, 20 hours |
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Applications |
The TG mice were injected with MG-262 or vehicle 20 h before the tissue samples were collected. MG-262 inhibited chymotryptic activity in the heart, lungs, skeletal muscle, and liver by 50–75%. GFPdgn protein abundance in all the major organs showed responsive increases upon systemic proteasomal inhibition induced by MG-262. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Zavrski I, Krebbel H, Wildemann B, et al. Proteasome inhibitors abrogate osteoclast differentiation and osteoclast function. Biochemical and biophysical research communications, 2005, 333(1): 200-205. [2] Kumarapeli A R K, Horak K M, Glasford J W, et al. A novel transgenic mouse model reveals deregulation of the ubiquitin-proteasome system in the heart by doxorubicin. The FASEB journal, 2005, 19(14): 2051-2053. | |
| Cas No. | 179324-22-2 | SDF | |
| Synonyms | PS-III,MG262,MG 262 | ||
| Chemical Name | [(1R)-3-methyl-1-[[(2S)-4-methyl-2-[[(2S)-4-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]pentanoyl]amino]butyl]boronic acid | ||
| Canonical SMILES | B(C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1)(O)O | ||
| Formula | C25H42BN3O6 | M.Wt | 491.44 |
| Solubility | ≥ 24.57mg/mL in DMSO, ≥ 96.4 mg/mL in EtOH | 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 | 2.0348 mL | 10.1742 mL | 20.3484 mL |
| 5 mM | 0.407 mL | 2.0348 mL | 4.0697 mL |
| 10 mM | 0.2035 mL | 1.0174 mL | 2.0348 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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