• Home
  • Search Results
  • Synthesis of bisboron compounds and their strong inhibitory activity on store-operated calcium entry.

Synthesis of bisboron compounds and their strong inhibitory activity on store-operated calcium entry.

Bioorganic & medicinal chemistry letters (2010-01-26)
Akinobu Z Suzuki, Shoichiro Ozaki, Jun-Ichi Goto, Katsuhiko Mikoshiba
ABSTRACT

Store-operated calcium entry (SOCE) is an important mechanism for replenishing intracellular calcium stores and for sustaining calcium signaling. We developed a method for synthesis of bisboron compounds that have two borinic acids or their esters in one molecule. These compounds are analogues of 2-APB, which is widely used as a membrane-permeable SOCE inhibitor. Further, we examined the effect of the newly synthesized bisboron compounds on SOCE in Jurkat T cells. All the bisboron compounds showed strong inhibitory activity on SOCE, with IC50 values of less than 1 microM, which were 20-45 times lower than observed with 2-APB.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
2-Aminoethyl diphenylborinate, 97%