Clathrin Inhibitor

ES9-17 is an analog of ES9 (endosidin9), which is an inhibitor of clathrin heavy chain (CHC). ES9-17 is an inhibitor of clathrin-mediated endocytosis (CME), a major route for internalization of plasma membrane proteins and molecules from the extracellular environment in plants. ES9-17 inhibits the uptake of transferrin and FM4-64. ES9-17 also inhibits root growth of Arabidopsis seedings.

Pitstop 2d is a Clathrin inhibitor with an IC₅₀ of <2 μM. Pitstop 2d binds to Clathrin N-terminal β-propeller domain, inhibits Clathrin function and dynamics and impairs VSV entry. Pitstop 2d inhibits Clathrin-mediated Endocytosis. Pitstop 2d does not inhibit clathrin-independent Endocytosis.

Pitstop 2c is a clathrin terminal domain inhibitor with an IC₅₀ of 1.8 μM. Pitstop 2c blocks the binding of epsin 1 to the clathrin terminal domain and impairs epsin 1-mediated membrane curvature formation at the early stage of clathrin-mediated endocytosis (CME). Pitstop 2c enhances the clathrin-independent endocytosis of galectin-3 and alters its intracellular distribution. Pitstop 2c causes mild defects in lysosomal acidification, as well as a slight increase in mitochondrial number but a reduction in average mitochondrial size. Pitstop 2c can be used in studies related to vesicular stomatitis virus infection.

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