JTE-013

JTE-013 is a potent and selective small molecule antagonist of the sphingosine-1-phosphate receptor 2 (S1P2, also known as EDG-5). It exhibits high affinity with IC50 values of approximately 17 nM for human S1P2 and 22 nM for rat S1P2. By blocking S1P2 receptors, JTE-013 inhibits downstream G-protein coupled receptor signaling pathways involved in inflammation, immune response, and cell proliferation/migration. Preclinical research has explored its potential in various conditions, including hepatocellular carcinoma, colorectal cancer, neuroblastoma, glioblastoma multiforme, and diabetic erectile dysfunction. It is currently utilized primarily as a research tool and has not advanced to clinical trials in humans.

Other names

1-(2,6-dichloropyridin-4-yl)-3-[(1,3-dimethyl-4-propan-2-ylpyrazolo[3,4-b]pyridin-6-yl)amino]urea