Biological ActivityAY 254 is a potent PAR2 biased agonist. Selectively activates ERK1/2 signaling (EC50 = 2 nM for ERK1/2 phosphorylation versus 80 nM for Ca2+ release). Reduces cytokine-induced caspase 3/8 activation, promotes scratch-wound healing, and induces IL-8 secretion, in human colorectal cancer (HT29) cells in vitro.
(Modifications: X-1 = 5-Isoxazolylcarbonyl-Cha, X-2 = Chg, Arg-4 = C-terminal amide)
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Biased signaling by agonists of protease activated receptor 2.
Jiang et al.
ACS Chem.Biol., 2017;12:1217
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