clathrin-mediated endocytosis

ES9-17, an analog of ES9 (endosidin9), is an inhibitor of clathrin-mediated endocytosis (CME). ES9-17 inhibits the uptake of FM4-64 and transferrin. ES9-17 inhibits root growth of Arabidopsis seedings.

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).

Ikarugamycin, an antibiotic, is an inhibitor of clathrin-mediated endocytosis (CME).

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.

Pyrimidyn 7 is an inhibitor of dynamin I II (dynaminI II) with IC50 values of 1.1 μM and 1.8 μM, respectively. It competitively inhibits the interaction between GTP and phospholipids with dynamin I (dynaminI). Additionally, Pyrimidyn 7 reversibly inhibits clathrin-mediated endocytosis (CME) of transferrin and epidermal growth factor (EGF) in various non-neuronal cells.

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.

2H-Cho-Arg is a steroid-based cationic lipid that contains a 2H-cholesterol skeleton coupled to an L-arginine head group and can be used to facilitate gene transfection. It forms a complex with plasmid DNA (pDNA) and decreases pDNA migration in an electrophoretic mobility shift assay at +/- charge ratios of 4 or higher. 2H-Cho-Arg facilitates transfection of a luciferase gene into H1299 cells, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the caveolae-mediated endocytosis inhibitor genistein , but not by inhibitors of clathrin- or micropinocytosis-mediated endocytosis. It induces cytotoxicity in H1299 cells (IC50 = 92.7 μg/ml).

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.

Pitstop2 is an amphipathic protein-bound inhibitor of the clathrin terminal domain (IC50=12 μM) with selectivity. Pitstop2 severely interferes with receptor-mediated endocytosis, HIV entry and synaptic vesicle cycling. Pitstop2 has antitumor activity.

Clathrin-IN-1 is a inhibitor of clathrin, and inhibits clathrin-mediated endocytosis (CME) by associating with the terminal domain of clathrin. It has the potential for anti-cancer research.