| 应用 |
A proteasome and NF-κB inhibitor. |
| 产品介绍 |
MG-132是一种蛋白酶体抑制剂，IC50为100 nM，也抑制钙蛋白酶，IC50为1.2 μM。 |
| 备注 |
MG-132 is an inhibitor of proteasome with IC50 of 100 nM, and also inhibits calpain with IC50 of 1.2 μM. |
| 生化机理 |
MG-132 [Z-Leu-Leu-Leu-CHO] is a proteasome inhibitor, used as a tool for perturbing the proteasome-regulated degradation of intracellular proteins. These proteins processed by the proteasome are involved in inflammatory processes and cell cycle regulation, presenting broad relevance for aldehydic proteasome inhibitors of this type. MG-132 suppresses NF-κB activation (at 10 μM) by preventing IκB degradation (IC50=3 μM), which blocks the transcription factor from providing chemoresistance to cancer cells. It is also an an inhibitor of calpain. MG-132 [Z-Leu-Leu-Leu-CHO] is an inhibitor of 26S Proteasome and an activator of JNK1, c-Jun and c-Fos. |
| 别名 |
MG132;蛋白酶体抑制剂; N-[(苄氧基)羰基]-L-亮氨酰-N-[(1S)-1-甲酰基-3-甲基丁基]-L-亮氨酰胺;Z-Leu-Leu-Leu-al;Carbobenzoxy-L-leucyl-L-leucyl-L-leucinal;Calpain inhibitor IV-2; N-[(Phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide |
