生物活性 | |||
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描述 | Aspartic proteinases are a class of enzymes commonly expressed in osteoclasts that contribute to bone resorption in endosome/lysosome system. Pepstatin A is a chemotactic pentapeptide that inhibits different kinds of aspartic proteinases, such as pepsin, cathepsins D and E. In a co-culture system, Pepstatin A at 15 - 120 μM suppressed the formation of TRAP-positive multinuclear cells in a dose-dependent manner. Pepstatin A at the same concentration range also exhibited a similar inhibitory effect on RANKL/M-CSF-induced osteoclastogenesis in bone marrow culture. In bone marrow cells separated from stromal cells on a Sephadex G-10 column, pepstatin A at 15 - 120 μM dose-dependently suppressed RANKL-induced osteoclastogenesis. In osteoclasts generated from bone marrow cells and stimulated with RANKL and M-CSF, pepstatin A at 120 μM strongly inhibited the early stage of osteoclast formation. Pepstatin A at 15 μM sufficiently inhibited the aspartic proteinase activity in bone marrow cells and the complete inhibition was seen at the concentration of 90 μM. Additionally, pretreatment of pepstatin A for 3 hours inhibited RANKL-induced ERK activation and NFATc1 expression in osteoclasts[3]. Pepstatin A stimulated human neutrophil degranulation and superoxide production with EC50 values of 0.75 μM and 1.5 μM respectively[4]. |
细胞研究 | |||||
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细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
human MCF7 cells | Function assay | Inhibition of cathepsin D in human MCF7 cells by fluorescence assay, IC50=0.005 μM | 19715320 | ||
human MCF7 cells | Function assay | 1 h | Inhibition of cathepsin D in human MCF7 cells treated for 1 hr measured after washout and trypsin treatment by fluorescence assay, IC50=5 μM | 19715320 |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.46mL 0.29mL 0.15mL |
7.29mL 1.46mL 0.73mL |
14.58mL 2.92mL 1.46mL |
参考文献 |
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