(R)-MG132 ((S,R,S)-(-)-MG-132) 是 MG-132 的对映异构体。 (R)-MG132 是一种蛋白酶体抑制剂，其细胞毒性比 MG-132 弱。 (R)-MG132 立体异构体是比 MG-132 更有效的蛋白酶体抑制剂。
| Cas No. | 1211877-36-9 |
| 别名 | N-[(苯基甲氧基)羰基]-L-亮氨酰-N-[(1S)-1-甲酰基-3-甲基丁基]-D-亮氨酰胺,(S,R,S)-(-)-MG-132; Z-Leu-D-Leu-Leu-al |
| 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 |
| 分子式 | C26H41N3O5 |
| 分子量 | 475.6 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 25 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 文献引用 | |
| 产品描述 | The ubiquitin-proteasome pathway plays an integral role in the selective degradation of intracellular proteins. While important for clearing damaged or mis-folded proteins, this proteolytic pathway also regulates the availability of key proteins involved in the control of inflammatory processes, cell cycle regulation, and gene expression. (R)-MG132 is a potent, reversible, and cell permeable proteasome inhibitor. After treatment for one hour at 100 nM, it inhibits 50% and 31% of proteasome activity in lysates of J558L multiple myeloma cells and EMT6 breast cancer cells, respectively. The (R)-MG132 stereoisomer is a more effective inhibitor of chymotrypsin-like (ChTL), trypsin-like (TL), and peptidylglutamyl peptide hydrolyzing proteasome (PGPH) activities compared to (S)-MG132 (IC50s = 0.22 versus 0.89 µM (ChTL); 34.4 versus 104.43 µM (TL); 2.95 versus 5.70 µM (PGPH), respectively). |
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