| Bioactivity | 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[1][2]. | ||||||||||||
| Invitro | ES9-17 (0-100 μM; 30 分钟) 抑制亲脂性苯乙烯基内吞示踪剂 (FM4-64) 的吸收，EC50 为 13 μM[1]。ES9-17 (30 μM; 30分钟) 不会消耗拟南芥细胞的 ATP[1]。ES9-17 (30 μM; 30分钟) 也降低了 HeLa 细胞中转铁蛋白的摄取[1]。ES9-17 靶向 CHC，调控内膜运输途径，不引起细胞质酸化[2]。 | ||||||||||||
| Name | ES9-17 | ||||||||||||
| CAS | 55854-43-8 | ||||||||||||
| Formula | C10H8BrNO2S2 | ||||||||||||
| Molar Mass | 318.21 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [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. |