Description
An inhibitor of SPHK1 and SPHK2 (Kis = 27 and 6.9 µM, respectively); selective for SPHK1/2 over a panel of 140 human protein kinases at concentrations up to 25 µM; reduces generation of cellular S1P without inducing SPHK1 degradation in Jurkat cells; induces a 3.7-, 3.5-, and 5.8-fold increase in C-18 ceramide, C-20 ceramide, and C20:1-ceramide levels, respectively; reduces proliferation of a variety of human cancer cell lines (EC50s = 8-44.9 µM); reduces tumor vasculature and volume as well as S1P protein levels in A549 human lung adenocarcinoma xenografts in mice