Mdivi 1

线粒体分裂抑制剂；50µM时抑制酵母Dnm1（重组酶的IC50=~1-10µM）和人类A549细胞中的DRP1的GTPase活性；50µM时抑制过表达DRP1的COS细胞中星形孢菌素诱导的线粒体碎裂和DRP1自组装；25和50µM时分别诱导A549细胞凋亡并抑制其集落形成；1µM时降低Langendorff离体灌注大鼠心脏缺血再灌注损伤模型中阿霉素诱导的梗塞风险比增加；20mg/kg时降低LPS诱发的急性肺损伤小鼠模型中肺损伤的严重程度。A mitochondrial division inhibitor; inhibits the GTPase activity of yeast Dnm1 (IC50 = ~1-10 µM for the recombinant enzyme) and human DRP1 in A549 cells at 50 µM; inhibits staurosporine-induced mitochondrial fragmentation and DRP1 self-assembly in COS cells overexpressing DRP1 at 50 µM; induces apoptosis in, and inhibits colony formation of, A549 cells at 25 and 50 µM, respectively; decreases doxorubicin-induced increases in infarct-to-risk ratios in a Langendorff isolated perfused rat heart model of ischemia-reperfusion injury at 1 µM; reduces the severity of lung injury in a mouse model of LPS-induced acute lung injury at 20 mg/kg.