SKI-II

Selective, non-ATP competitive inhibitor of sphingosine kinase (IC₅₀ = 0.5µM GST-hSK; IC₅₀ = 1.1µM intact JC mouse mammary adenovirus carcinoma cells) showing no inhibition of hERK2, hPI3k and hPKCα at concentrations up to 60µM. Cytotoxic effects have been demonstrated against various tumor cell lines including some overexpressing P-glycoprotein or MRP1 (T24, IC₅₀ = 4.6µM; MCF-7, IC₅₀ = 1.2µM; NCI/ADR, IC₅₀ = 1.3µM, MCRF-7/VP, IC₅₀ = 0.9µM). Induced apoptosis in T24 tumor cells.