In order to obtain compounds with modified 2-APB activities, we synthesized number of bis-boron 2-APB analogues and analyzed their inhibitory activities for SOCE and IICR. Adducts of amino acids with bis-borinic acid showed the highest activity. The IC50 of 2-APB for SOCE inhibition was 3 µM, while the IC50 of 2051 bis(4,4'(phenyllysineboryl)benzyl) ether was 0.2 µM. By using these compounds, we may be able to regulate Ca2+ release and consequent cellular processes more efficiently than with 2-APB.
Keywords: 2-APB, 2-APB analogue, regulator of Ca2+ release, regulator of cellular processes