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ABC294640 is a selective and competitive inhibitor of sphingosine kinase 2 (SK2) with IC50 value of 60μM [1].

ABC294640 is a competitive inhibitor of SK2. It shows IC50 value of about 60μM against recombinant human SK2. In the kinetic assay, ABC294640 competes with sphingosine and exerts a Ki value of 9.8μM. Because of its targeting of the sphingosine binding site of SK2, ABC294640 shows no inhibition activity against other 20 kinases. In MDA-MB-231 cells, ABC294640 prevents S1P production with IC50 value of 26μM. Moreover, ABC294640 has anti-proliferation and anti-migration efficacies in tumor cells. It suppresses cell proliferation of a variety of tumor cell lines such as 1025LU, A-498, Caco-2 and HT-29. The IC50 values are ranged from 6μM to 48μM. Furthermore, administration of ABC294640 inhibits tumor growth in the immunocompetent BALB/c mice bearing mammary adenocarcimona xenografts. Besides that, ABC294640 is also found to have greater anti-proliferation effects in ER-positive than ER-negative breast cancer cells. The effect of E2 signaling caused by ABC294640 is expected to be a therapeutic in endocrine-related diseases [1, 2].

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