I-191 is a novel potent, selective protease-activated receptor 2 (PAR2) antagonist with pIC50 of 7.2 in cell-based assays.
I-191 potently attenuates multiple PAR2-mediated intracellular signaling pathways leading to Ca2+ release, ERK1/2 phosphorylation, Ras homologue gene family, member A (RhoA) activation, and inhibition of forskolin-induced cAMP accumulation.
I-191 also potently inhibits PAR2-mediated downstream functional responses, including expression and secretion of inflammatory cytokines and cell apoptosis and migration, in human HT29 and MDA-MB-231 cells.
