1-[2-(1-Benzyl-2,5-dimethyl-1H-pyrrol-3-yl)-2-oxo-ethyl]-6-oxo-1,6-dihydro-pyridine-3-carbonitrile

Description

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.

Uses

CYM-5520 has been used as a sphingosine 1-phosphate receptor 2 (S1pr2) agonist in pancreatic adenocarcinoma?cell?line (CFPAC-1).

Biochem/physiol Actions

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.

storage

Store at +4°C