E4031

E4031 is a methanesulfonanilide small molecule that acts as a potent and selective blocker of the human ether-à-go-go-related gene (hERG) potassium channel, specifically targeting the rapid component of the delayed rectifier potassium current ($I_{Kr}$). Originally developed by Eisai as an experimental Class III antiarrhythmic agent, it is now primarily utilized as a high-affinity research tool in electrophysiology and oncology. In cancer research, E4031 is used to investigate the role of hERG1 channels in tumor progression, cell migration, and force transduction, as these channels are often overexpressed in various malignancies, including pancreatic ductal adenocarcinoma. Due to its potent inhibition of hERG, which can lead to QT interval prolongation, it is also frequently used in safety pharmacology to model drug-induced Long QT syndrome.

Other names

1-[2-(6-methyl-2-pyridyl)ethyl]-4-(methylsulfonylaminobenzoyl)piperidine