Dyngo-4a

一种动力蛋白抑制剂（天然羊脑动力蛋白1和重组大鼠动力蛋白2的IC50分别为380和2,300nM）；抑制PS脂质体诱导的动力蛋白1螺旋形成(IC50=0.38µM)的效果优于抑制Grb2诱导的单环动力蛋白1形成(IC50=39.2µM)；不抑制动力蛋白的基础GTPase活性；抑制非神经元网格蛋白介导的(U2OS细胞中IC50=5.7µM)和突触小泡内吞作用(大鼠脑突触体中IC50=26.8µM)。An inhibitor of dynamin (IC50s = 380 and 2,300 nM for native sheep brain dynamin 1 and recombinant rat dynamin 2, respectively); inhibits PS liposome-induced dynamin 1 helix formation (IC50 = 0.38 µM) more potently than Grb2-induced single-ring dynamin 1 formation (IC50 = 39.2 µM); does not inhibit the basal GTPase activity of dynamin; inhibits non-neuronal clathrin-mediated (IC50 = 5.7 µM in U2OS cells) and synaptic vesicle endocytosis (IC50 = 26.8 µM in rat brain synaptosomes).