I-287 is a selective, orally active PAR2 inhibitor that functions as a negative allosteric modulator of Gαq and Gα12/13 activity and their downstream effectors. It has been shown to attenuate Complete Freund's adjuvant-induced inflammation in mice, suggesting its utility in inflammation/immunology research [1].

I-287 (0-60 μM; 15-30 minutes) inhibits PAR2-mediated activation of Gαq and Gα12/13 proteins in HEK-293 cells without affecting Gi/o proteins and does not impact β-arrestin 2 recruitment or receptor internalization [1]. Additionally, I-287 (0-60 μM; 15-30 minutes) suppresses PAR2-mediated ERK1/2 activation [1]. At 10 μM for 30 minutes, I-287 also inhibits PAR2-induced IL-8 secretion in HCT-116 and A549 cells [1].

I-287 (orally administered at a dosage of 50 mg/kg) reduced the inflammatory response induced by Complete Freund's adjuvant in C57BL/6J mice [1].