Description
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, S1P
1/EDG-
1, S1P
2/EDG-
5, S1P
3/EDG-
3, S1P
4/EDG-
6, and S1P
5/EDG-
8. JTE-
013 is a potent, selective sphingosine-
1-
phosphate 2 (S1P
2) receptor antagonist that binds to the human and rat receptors with IC
50 values of 17 and 22 nM, respectively, (IC
50 values >10 μM for human S1P
1 and S1P
3). 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.
Definition
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.
