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Description

A cell-permeable disubstituted thiazole compound that displays anti-tumor properties. Acts as a potent, substrate competitive, reversible, and highly specific inhibitor of sphingosine kinase (IC50 = 0.5 µ,M for GST-hSK). Does not affect the kinase activity of hERK2, hPI3K, or PKCalpha even at concentrations as high as 60 µ,M. Induces apoptosis in human cancer cells that express the drug transport proteins Pgp or MRP1 (IC50 = ~ 1-5 µ,M) through inhibiting sphingosine-1-phosphate production., A cell-permeable, potent non-ATP-competitive, reversible, and specific inhibitor of sphingosine kinase (IC50 = 500 nM for GST-hSK) that also exhibits anti-tumor properties. Does not affect the kinase activity of hERK2, hPI3 K, or PKCalpha at cocentrations as high as 60 µ,M. Shown to induce apoptosis in human cancer cells that express the drug transport proteins Pgp or MRP1 (IC50 ~1-5 µ,M) by inhibiting sphingosine-1-phosphate production.