JTE-013 is a potent and specific S1P₂ (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P₂ with IC₅₀s of 17 nM and 22 nM, respectively^[1]. IC50 & Target: IC50: 17 nM (S1P₂ for human) and 22 nM (S1P₂ for rat)^[1] In Vitro: JTE-013 (50-200 μM; 1-3 days) reduced cell viability^[1].
JTE-013 (10-1000 nM; 30 mins) reverses S1P-induced Akt inhibition and inhibits S1P-induced ERK activation^[1].
JTE-013 displays 4.2% inhibition of S1P₃ and does not antagonize S1P₁ at concentrations up to 10 μM^[1]. In Vivo: JTE-013 (gavage; 30 mg/kg daily for 14 consecutive days) reduces tumor size and tumor weight^[1].