Sphingosine-1-phosphate (S1P; ) is an extracellular lipid mediator whose major effects are mediated through five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8. S1P2 has been implicated in multiple biological functions, including Rho activation, inhibition of Rac and cell migration, and in “feed forward” autocrine signaling in NF-κB survival signaling of tumor cells. CYM 5520 is a noncompetitive allosteric agonist of S1P2 (EC50 = 0.48 μM) that does not display agonist activity towards S1P1, S1P3, S1P4, or S1P5.
CYM-5520 is a specific, noncompetitive allosteric agonist of sphingosine 1-phosphate receptor 2 (S1PR2; EC50 = 1.0 μM). The compound CYM-5520 does not show any agonsit activity towards S1PR1, S1PR3, S1PR4 or S1PR5.