MG-262
(Synonyms: PS-III,MG262,MG 262) 目录号 : GC15517
A proteasome inhibitor with diverse biological activities
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 | |
| 别名 | PS-III,MG262,MG 262 | ||
| 化学名 | [(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 | ||
| 分子式 | C25H42BN3O6 | 分子量 | 491.44 |
| 溶解度 | ≥ 24.57mg/mL in DMSO, ≥ 96.4 mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet