Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis. It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8. JTE-013 is a potent, selective sphingosine-1-phosphate 2 (S1P2) receptor antagonist that binds to the human and rat receptors with IC50 values of 17 and 22 nM, respectively, (IC50 values >10 μM for human S1P1 and S1P3). It reverses the inhibitory effects of S1P on cell migration of vascular endothelial cells and smooth muscle cells. Similarly, JTE-013 reverses the inhibition of S1P on invasion and migration of B16 melanoma cells. JTE-013 inhibits S1P-induced contraction of, as well as cyclic AMP accumulation in, coronary artery smooth muscle cells.
ChEBI: 1-(2,6-dichloro-4-pyridinyl)-3-[(1,3-dimethyl-4-propan-2-yl-6-pyrazolo[3,4-b]pyridinyl)amino]urea is a pyrazolopyridine.
