MG-262
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
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
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
- 1. Andrew Thorne, Akanksha Bansal, et al. "Differential regulation of BIRC2 and BIRC3 expression by inflammatory cytokines and glucocorticoids in pulmonary epithelial cells." PLoS One. 2023 Jun 8;18(6):e0286783. PMID: 37289679
- 2. Fullbright G, Rycenga HB, et al. "p97 Promotes a Conserved Mechanism of Helicase Unloading during DNA Cross-Link Repair." Mol Cell Biol. 2016 Nov 14;36(23):2983-2994. PMID: 27644328
| Physical Appearance | A solid |
| Storage | Store at -20°CThe product is not stable in solution, please dissolve it immediately before use. |
| M.Wt | 491.44 |
| Cas No. | 179324-22-2 |
| Formula | C25H42BN3O6 |
| Synonyms | PS-III,MG262,MG 262 |
| Solubility | ≥24.57 mg/mL in DMSO; insoluble in H2O; ≥96.4 mg/mL in EtOH |
| Chemical Name | [(1R)-3-methyl-1-[[(2S)-4-methyl-2-[[(2S)-4-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]pentanoyl]amino]butyl]boronic acid |
| SDF | Download SDF |
| 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| 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. |
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| Description | MG-262 is a reversible and cell-permeable proteasome inhibitor. | |||||
| Targets | proteasome | |||||
| IC50 | 122 nM | |||||
Quality Control & MSDS
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Chemical structure
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