I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant -induced inflammation in mice and can be used for inflammation/immunology research.
I-287 (0-60 μM; 15-30 min) inhibits PAR2-mediated activation of Gαq and Gα12/13 but not Gi/o proteins while has no effect on PAR2-mediated recruitment of βarrestin2 and receptor internalization[1].I-287 (0-60 μM; 15-30 min) inhibits PAR2-mediated ERK1/2 activation in HEK293 cells[1].I-287 (10 μM; 30 min) inhibits PAR2-induced secretion of IL-8 cytokine in HCT-116 and A549 cells[1].
I-287 (50 mg/kg for p.o.) reduces Complete Freund's adjuvant -induced inflammation in C57BL/6J mice[1].
References:
[1]. Avet C, et.al. The PAR2 inhibitor I-287 selectively targets Gαq and Gα12/13 signaling and has anti-inflammatory effects. Commun Biol. 2020 Nov 27;3(1):719.