DRP1i27 is a novel inhibitor of human Drp1 (mitochondrial dynamin-related protein 1), directly binds to and inhibits GTPase activity of human Drp1.
DRP1i27 induced both significant reduction in cell death induced by hydrogen peroxide treatment and a significant increase in the percentage of cells with elongated mitochondria.
DRP1i27 shows dose-response binding to human Drp1 isoform 3 with a KD of 286 (SPR) and KD of 190.9 uM (MST).
DRP1i27 5-50 µM showed a trend of inhibition of the conversion of GTP to GDP in the GTPase activity assay.
DRP1i27 targets Drp1-mediated mitochondrial fission in cell line models and protects against simulated ischemia–reperfusion injury.
