生物活性 | |||
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描述 | The heme enzyme myeloperoxidase (MPO) participates in innate immune defense mechanism through formation of microbicidal reactive oxidants. MPO-IN-28 is a the first potent, selective and mechanism-based irreversible MPO inhibitor with IC50 value of 44nM. MPO-IN-28 achieved residual MPO activity without H2O2 by 84%, residual MPO activity with H2O2 by 4%, residual MPO activity with Cl−+ H2O2 by 5% at 5μM and inhibited LDL oxidation with IC50 value of 0.09μM. It dose-dependently inhibited MPO inside neutrophils with IC50 value of 93.1μM. MPO-IN-28 possesses the characteristic of blood−brain barrier permeability, human intestinal absorption and cell permeability. It inhibited in vitro growth of normal human dermal fibroblast with IC50 value 17μM[2]. | ||
作用机制 | MPO-IN-28 interacts with the active site of MPO and MPO uses hydrogen peroxide to oxidize MPO-IN-28 thereby irreversibly inactivating the enzyme.[2] |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.32mL 0.86mL 0.43mL |
21.62mL 4.32mL 2.16mL |
43.24mL 8.65mL 4.32mL |
参考文献 |
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