Cysteine proteases play multiple roles in basically all aspects of physiology and development. Furthermore, they are engaged in signalling pathways and in the response to biotic and abiotic stresses[3]. Aloxistatin is a specific and potent inhibitor of cysteine proteinases isolated from a culture of Aspergillus japonicus[3]. Aloxistatin at a series of concentrations was able to enter the intact platelet and inhibit the protease activity in lysed platelets when incubated for 5 min[4]. After a brief preincubation with the membrane-permeable, Aloxistatin (10 mg/ml) blunted PTH-induced (parathyroid hormone) cell proliferation in sub-confluent cultures and also attenuated proliferation and inhibited differentiation in longer-term confluent cultures[5]. Aloxistatin(100 mg/kg, p.o.) inhibited the activity of cathepsin B&L in skeletal muscle, heart, and liver of hamsters[6].
作用机制
Aloxistatin reacts irreversibly with the thiol group at the active site.
E-64d 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
U937 cells
Function assay
Blockade of cathepsin G processing in human U937 cells by densitometry, IC50=1.1 μM
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