endocytosis,dynamin,gtpase

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).

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 I inhibitor

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.

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.

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.

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