| Description |
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].
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| Related Catalog |
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| Target |
IC50: 17 nM (S1P2 for human) and 22 nM (S1P2 for rat)[1]
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| 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]. Cell Viability Assay[1] Cell Line: SK-N-AS cells Concentration: 50, 100, 150, 200 μM Incubation Time: 1-3 days Result: Reduced cell viability. Western Blot Analysis[1] 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.
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| In Vivo |
JTE-013 (gavage; 30 mg/kg daily for 14 consecutive days) reduces tumor size and tumor weight[1]. Animal Model: Six-week-old female athymic NCr-nu/nu nude mice[1] Dosage: 30 mg/kg Administration: Gavage; daily for 14 consecutive days Result: Reduced tumor size and tumor weight.
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| References |
[1]. Li MH, et al. Antitumor Activity of a Novel Sphingosine-1-Phosphate 2 Antagonist, AB1, in Neuroblastoma. J Pharmacol Exp Ther. 2015 Sep;354(3):261-8.
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