Cell-permeable version of dynamin inhibitory peptide, an inhibitor of the GTPase dynamin that competitively blocks binding of dynamin to amphiphysin, preventing endocytosis. Reduces NMDA receptor internalization.
Dynamin-related GTPase DRP1 partial inhibitor (IC50 = 1.2 μM). Selective for DRP1 over other dynamin-related GTPases, OPA1 and DYN1. Increases mitochondrial DNA levels in mfn1- knockout MEFs deficient in mitochondrial fusion.
Mallat et al (2018) Discovery and characterization of selective small molecule inhibitors of the mammalian mitochondrial division dynamin, DRP1. Biochem.Biophys.Res.Commun. 499 556 PMID:29601815
Ellipticine quinone, also known as NSC-383230, is a Drp1 inhibitor. rpitor1 and Drpitor1a inhibited the GTPase activity of Drp1 without inhibiting the GTPase of dynamin 1. Ellipticine quinone showed greater potency than the current std. Drp1 GTPase inhibitor, mdivi-1, (IC50 for mitochondrial fragmentation are (0.06, and 10 μM, resp.). Ellipticine quinone suppressed lung cancer tumor growth in a mouse xenograft model. Ellipticine quinone also inhibited mitochondrial ROS prodn., prevented mitochondrial fission, and improved right ventricular diastolic dysfunction during IR injury.