MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM).
Calpain is a calcium-activated protease with exist as an inactive proenzyme in the cytosol. When intracellular calcium level is overloaded, it triggers to convert the proenzyme to its active form. Activated calpain then cleaves xytoplasmiv and nuclear substrates, leading to apoptosis[3]. In transgenic models, the absence of cathepsin B has been associated with enhanced apoptosis, yet cathepsin B also has been shown to contribute to apoptosis. Cathepsin B is part of a proteolytic pathway identified in xenograft models of human glioma; targeting only cathepsin B in these tumors is less effective than targeting cathepsin B in combination with other proteases or protease receptors[4].
MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively[5]. Experiment showed that MG-101 (given at 5, 10, or 20mg/kg i.p. in the pleurisy model or at 5mg/kg i.p. every 48 hours in the arthritis model) exerts potent anti-inflammatory effects in vivo and reduced the staining for nitrotyrosine and poly (ADP-ribose) polymerase[6].
MG-101 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
HEK293 cells
Function assay
Effect on cofilin1 expressed in HEK293 cells assessed as effect on cofilin1; Limk2 interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay
16680159
HeLa cells
Cytotoxicity assay
48 h
Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by MTS assay, CC50=25.1 μM
23357632
L1210 cells
Function assay
Inhibitory concentration of the compound was determined against L1210 cells, IC50=3 μM
15634028
melanoma B16 cells
Function assay
Inhibitory concentration of the compound was determined against melanoma B16 cells, IC50=14.5 μM
Effect on cofilin1 expressed in HEK293 cells assessed as effect on cofilin1; Limk2 interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay
16680159
HeLa cells
Cytotoxicity assay
48 h
Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by MTS assay, CC50=25.1 μM
23357632
L1210 cells
Function assay
Inhibitory concentration of the compound was determined against L1210 cells, IC50=3 μM
15634028
melanoma B16 cells
Function assay
Inhibitory concentration of the compound was determined against melanoma B16 cells, IC50=14.5 μM
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