gtpase dynamin

Mdivi-1 (Mitochondrial division inhibitor 1) is a mitochondrial division inhibitor that inhibits DRP1 and Dynamin I (IC50=1-10 μM). Mdivi-1 inhibits mitochondrial autophagy.

Dynamin IN-2 (compound 43) is a Wiskostatin analogue. Dynamin IN-2 is a potent dynamin inhibitor (dynamin I GTPase, IC50= 1.0 μM). Dynamin IN-2 blocks clathrin mediated endocytosis (CME) (IC50= 9.5 μM).

Tetradecyltrimethylammonium bromide (MitMAB) is a Dynamin GTPase activity inhibitor and a cationic surfactant with asymmetrical structure.

Dynasore (Dynamin Inhibitor I), a cell-permeable chemical, can reversibly and non-competitivity inhibit GTPase activity of dynamin 1 2 (IC50: 15 μM in a cell-free assay). It also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase.

Hydroxy-Dynasore (Dyngo-4a) , a effective dynamin inhibitor, inhibits withDynI (brain), DynI (rec), and DynII (rec) of IC50 of 0.38 μM, 1.1 μM, and 2.3 μM, respectively.

Dynamin inhibitory peptide Acetate is a peptide with the sequence Gln-Val-Pro-Ser-Arg-Pro-Asn-Arg-Ala-Pro that inhibit the GTPase dynamin.

Dynamin I inhibitor

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

RTIL 13 is a highly effective inhibitor of dynamin GTPase, exhibiting an IC50 value of 2.3 μM for dynamin I GTPase. Furthermore, it selectively interacts with the pleckstrin homology lipid binding domain. This compound effectively suppresses both receptor-mediated and synaptic vesicle endocytosis, demonstrating IC50 values of 9.3 μM and 7.1 μM, respectively.

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.

Clathrin-IN-2 is a potent inhibitor of clathrin-mediated endocytosis (CME), demonstrating an IC50 value of 2.3 μM. Additionally, it exhibits inhibitory effects on dynamin I GTPase, with an IC50 of 7.7 μM.

DRP1i27, a potent human dynamin-related protein 1 (Drp1) inhibitor, targets the GTPase site of Drp1, forming hydrogen bonds with Gln34 and Asp218. It mitigates Drp1-mediated mitochondrial fission in cell line models and offers protection against simulated ischemia-reperfusion injury.

MiTMAB, a selective dynamin inhibitor, targets the interaction between dynamin and phospholipids. This inhibitor can inhibit dynamin GTPase activity with a Ki value of 940 nM.

Sulfonadyn-47 is a dynamin inhibitor that effectively inhibits dynamin GTPase activity with an IC50 of 3.5 µM in cell-free assays. Additionally, it disrupts clathrin-mediated endocytosis in U2OS cells (IC50 = 27.3 µM) and impedes the depolarization-stimulated uptake of the synaptic vesicle endocytosis (SVE) marker FM4-64 in isolated rat brain synaptosomes (IC50 = 12.3 µM). Significantly, in vivo administration of sulfonadyn-47 at doses of 30 and 60 mg/kg demonstrates anticonvulsant properties in the 6 Hz corneal kindling mouse model of seizures.

Rhodady C10 (Compound C10) functions as an inhibitor of dynamin I GTPase. It effectively blocks receptor-mediated endocytosis (IC50: 7 μM), a process involving dynamin in clathrin-independent endocytosis, phagocytosis, and caveolae internalization.

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 protein 1 (Drp1) inhibitor, inhibits Drp1 GTPase activity. Displays no effect on dynamin 1 or other mitochondrial dynamics-related proteins. Inhibits mitochondrial fission, dysfunction and reactive oxygen species (ROS) production in vitro.

P110 TFA is a dynamin-related protein 1 (Drp1) inhibitor, inhibits Drp1 GTPase activity.

Control peptide version of dynamin inhibitory peptide, myristoylated, an inhibitor of the GTPase dynamin that competitively blocks binding of dynamin to amphiphysin, preventing endocytosis. In contrast to dynamin inhibitory peptide, has no significant eff