Use of Naphthalene-1,4-diketone compound as hCBS enzyme inhibitor

摘要

The use of a naphthalene-1,4-diketone compound as a human cystathionine β-synthase (hCBS) enzyme inhibitor, particularly relates to a use of the compound 2-chloro-3-(4-methylpiperazin-1-y1) naphthalene-1,4-dione as an hCBS enzyme inhibitor. The IC50 of the small molecule compound for in vitro hCBS enzyme assay is 20 µM. Such small molecule compound can be used as a drug tool for studying H2S signalling pathways, and as a lead compound for developing the drugs for treating the H2S related diseases, such as circulatory shock, stroke, Down's syndrome, and tumour, etc. In another aspect, a method for inhibiting in vitro hCBS 2-chloro-3-(4-methylpiperazin-1-y1) naphthalene-1,4-dione, said method involving the detection of H2S. In another aspect, a method for inhibiting the activity of the intracellular hCBS enzyme using 2-chloro-3-(4-methylpiperazin-1-y1) naphthalene-1,4-dione, the method involving the detection of H2S.