Bt2-Ins(1345)P4 / PM

Bt2-Ins(1,3,4,5)P4/PM is a membrane-permeant, bioactivatable derivative of myo-inositol 1,3,4,5-tetrakisphosphate (Ins(1,3,4,5)P4).

The negatively charged phosphate groups are masked by propionoxymethyl (PM) ester groups, while additional butyryl ester groups increase lipophilicity and facilitate cellular uptake. Following entry into cells, intracellular esterases cleave the ester groups, enabling intracellular delivery of Ins(1,3,4,5)P4.

Ins(1,3,4,5)P4 is an important regulator of cellular signaling and has been implicated in the regulation of calcium entry and phosphoinositide-dependent signaling. Membrane-permeant Bt2-Ins(1,3,4,5)P4/PM has been used experimentally to investigate the regulation of Orai1-mediated calcium entry, where application of the compound strongly inhibited open-state Orai1 currents.

Bt2-Ins(1,3,4,5)P4/PM is therefore suitable for cellular studies of InsP4 signaling, calcium entry and inositol phosphate-dependent regulation of signaling pathways.

References:

Miller A.T. et al., PLOS ONE 2015, 10, e0131071. DOI: 10.1371/journal.pone.0131071