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.
ES9-17 (0-100 渭M; 30 min) inhibits the uptake of the lipophilic styryl endocytic tracer dye (FM4-64), with an EC50 value of 13 渭M[1].
ES9-17 (30 渭M; 30 min) doesn鈥檛 deplete cellular ATP[1].
ES9-17 (30 渭M; 30 min) also reduces the uptake of transferrin in HeLa cells[1].
ES9-17 targets to CHC and mediates transport of materials among organelles without causing cytoplasmic acidification[1].
[1]. Dejonghe W, et al. Disruption of endocytosis through chemical inhibition of clathrin heavy chain function. Nat Chem Biol. 2019 Jun;15(6):641-649.
[2]. Huang L, et al. Progress in using chemical biology as a tool to uncover novel regulators of plant endomembrane trafficking. Curr Opin Plant Biol. 2019 Dec;52:106-113.