2093408-03-6

AY 254 is a potent PAR2 biased agonist. It selectively activates ERK1/2 signaling (EC50 = 2 nM for ERK1/2 phosphorylation versus 80 nM for Ca2+ release). AY 254 reduces cytokine-induced caspase 3/8 activation, promotes scratch-wound healing, and induces IL-8 secretion, in human colorectal cancer (HT29) cells in vitro.

AY254 is an analogue of AY77 (HY-138951). AY254 is ERK-biased PAR2 agonist with an EC50 of 2 nM. AY254 relieves cytokine-induced caspase 3/8 activation. AY254 also promotes scratch-wound healing and induced IL-8 secretion via PAR2-ERK1/2 signaling[1]

PAR2: 2 nM (EC₅₀)

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[1] Jiang Y, et al. Biased Signaling by Agonists of Protease Activated Receptor 2. ACS Chem Biol. 2017 May 19;12(5):1217-1226. DOI:10.1021/acschembio.6b01088