MG-132
基本信息
产品名称：
MG-132
英文名称：
MG-132
国产/进口：
进口
产地/品牌：
AmBeed
型号：
5mg
参考报价：
RMB220
销售商：
总点击数：
139
更新日期：
2025-01-22
产品类别：
性能参数
MG-132 is an inhibitor ofproteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 nM).
Proteasome and calpain are the main nonlysosomal proteases responsible for intracellular proteolysis. MG-132 is a potent cell-permeable inhibitor of both proteasome and calpain with respective IC50 values of 0.1µM and 1.25µM. MG-132 induced neurite outgrowth in PC12 cells at a concentration of 20nM. In rabbit erythrocytes, MG-132 penetrated cell membrane and inhibited the autolysis at the dose of 100µM[3]. MG-132 also showed inhibitory activity on cell growth in both human ocular melanoma IPC227F cells and murine melanoma B16 cells with IC50 values of 42 and 77nM, respectively[4]. In airway epithelial cells, pretreatment with 10μM MG-132 for 1h inhibited TNF-α-stimulated IL-8 protein production and release. Moreover, preincubation of cells with 10μM MG-132 reversed the effects of TNF-α on the transcriptional activity of IL-8 gene, IκB degradation, and NF-κB activation[5]. In mice with hindlimb immobilization, twice-daily subcutaneous injections of MG-132 (7.5 mg/kg/dose) significantly increased the running time on treadmill as compared to DMSO-treated group. However, no significant difference in the running time of MG132- and DMSO-treated mice was observed after 11 days of remobilization[6].
MG-132 inhibits proteasome primarily via acting on the chymotrypsin-like site in the subunit. It also inhibits the caspase-like site at high concentrations[7].
Proteasome and calpain are the main nonlysosomal proteases responsible for intracellular proteolysis. MG-132 is a potent cell-permeable inhibitor of both proteasome and calpain with respective IC50 values of 0.1µM and 1.25µM. MG-132 induced neurite outgrowth in PC12 cells at a concentration of 20nM. In rabbit erythrocytes, MG-132 penetrated cell membrane and inhibited the autolysis at the dose of 100µM[3]. MG-132 also showed inhibitory activity on cell growth in both human ocular melanoma IPC227F cells and murine melanoma B16 cells with IC50 values of 42 and 77nM, respectively[4]. In airway epithelial cells, pretreatment with 10μM MG-132 for 1h inhibited TNF-α-stimulated IL-8 protein production and release. Moreover, preincubation of cells with 10μM MG-132 reversed the effects of TNF-α on the transcriptional activity of IL-8 gene, IκB degradation, and NF-κB activation[5]. In mice with hindlimb immobilization, twice-daily subcutaneous injections of MG-132 (7.5 mg/kg/dose) significantly increased the running time on treadmill as compared to DMSO-treated group. However, no significant difference in the running time of MG132- and DMSO-treated mice was observed after 11 days of remobilization[6].
MG-132 inhibits proteasome primarily via acting on the chymotrypsin-like site in the subunit. It also inhibits the caspase-like site at high concentrations[7].
公司简介
AmBeed总部位于美国芝加哥,我们致力于为全球科学家提供高品质的活性小分子化合物,包括抑制剂、激动剂、天然产物、PROTACs、分子胶、ADC、配体及各类药物筛选库,其中涵盖大量能精确作用于各种靶点及其突变体的靶点特异性化合物,助您畅行精准医疗之路!
联系电话：400-920-2911
销售邮箱：sales@ambeed.cn
技术邮箱：tech@ambeed.cn
联系电话：400-920-2911
销售邮箱：sales@ambeed.cn
技术邮箱：tech@ambeed.cn
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