2-Aminoethyl diphenylborinate (2-APB) analogues: Regulation of Ca2+ signaling

Abstract

In order to obtain compounds with modified 2-APB activities, we synthesized number of 2-APB analogues and analyzed their inhibitory activities for SOCE. The IC50 of 2-APB for SOCE inhibition is 3μM while IC50 of some of our 2-APB analogues range 0.1–10μM. The adducts of amino acids with diphenyl borinic acid have strong inhibitory activities. By using these compounds, we will be able to regulate intracellular Ca2+ concentration and consequent cellular processes more efficiently than with 2-APB.