endocytosis,dynamin,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 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).

Dynasore (Dynamin Inhibitor I) is a highly selective, reversible small-molecule dynamin inhibitor with an IC₅₀ of 15 μM. Dynasore also inhibits the mitochondrial dynamin Drp1 without affecting other small GTPases. By inhibiting the GTPase activity of dynamin, Dynasore blocks its function in membrane fission, thereby inhibiting clathrin-mediated endocytosis. Dynasore can be used in research on endocytosis, membrane transport, viral entry, and receptor signaling regulation.

Clathrin-IN-5 (Compound 9) is an inhibitor of the Clathrin N-terminal domain and Amphiphysin protein-protein interactions, with an IC50 of 2.77 μM. It disrupts the interaction between the clathrin N-terminal domain and amphiphysin. Additionally, Clathrin-IN-5 inhibits clathrin-mediated endocytosis with an IC50 of 4.6 μM and suppresses Dynamin I's GTPase activity with an IC50 of 29.7 μM.

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