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.
性状
Solid
IC50 & Target[1][2]
IC50: 17 nM (S1P2 for human) and 22 nM (S1P2 for rat)
体外研究(In Vitro)
JTE-013 (50-200 μM; 1-3 days) reduced cell viability.
JTE-013 (10-1000 nM; 30 mins) reverses S1P-induced Akt inhibition and inhibits S1P-induced ERK activation.
JTE-013 displays 4.2% inhibition of S1P3 and does not antagonize S1P1 at concentrations up to 10 μM.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay
Cell Line:
SK-N-AS cells
Concentration:
50, 100, 150, 200 μM
Incubation Time:
1-3 days
Result:
Reduced cell viability.
Western Blot Analysis
Cell Line:
SK-N-AS cells
Concentration:
10, 100, 1000 nM
Incubation Time:
30 mins
Result:
Reversed S1P-induced Akt inhibition and inhibited S1P-induced ERK activation.
体内研究(In Vivo)
JTE-013 (gavage; 30 mg/kg daily for 14 consecutive days) reduces tumor size and tumor weight.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.