Dynasore is a cell-permeable, reversible non-competitive dynamin inhibitor of GTPase activity of dynamin 1/2, with IC50 of 15 μM in a cell-free assay, also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase.
Effects of dynasore on active caspase-3 expression at 3 days after SCI. c) Active caspase-3/NeuN/DAPI double labeling. Scale bars = 100 μm.
Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1) with IC50 of 1-10 μM.
A. shCon and shPINK1 cells were pretreated with Mdivi-1 (50 μM) for 2 h, followed by treatment with 8 μM PPI for 6 h. Mitochondrial fractions (Mito) were prepared and subjected to western blot analysis. B-C. RFP-mito-expressing cells were treated as indicated in (A), and fluorescence images were evaluated by confocal microscopy. Scale bars: 10 μm. Average mitochondrial length was quantified as previously described. Data are presented as mean ± SD (*P< 0.01 compared to shCon cells treated with PPI, ##P< 0.01 compared to shPINK1 cells treated with PPI). D-E. Cells were treated as indicated in (A); apoptosis was then measured by flow cytometry, and whole-cell lysates were prepared and subjected to western blot analysis. Data are presented as mean ± SD (*P< 0.01 compared to shCon cells treated with PPI, ##P< 0.01 compared to shPINK1 cells treated with PPI).
Dyngo-4a is a potent dynamin inhibitor with IC50 of 0.38 μM, 1.1 μM, and 2.3 μM for DynI (brain), DynI (rec), and DynII (rec), respectively.