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

•We synthesized number of 2-APB analogues.•We have measured SOCE and IICR and studied the structure–activity relation.•Adducts of amino acids with diphenyl borinic acid gave strongest inhibitory activities.•911 Diphenyl(2,6-diaminohexanateO,N)borane, is the best compound. 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.