Your company account is blocked and you cannot place orders. If you have questions, please contact your company administrator.

Development of a sphingosine kinase 1 specific small-molecule inhibitor.

Basic Information

ID: ALA1287751

Journal: Bioorg Med Chem Lett

Title: Development of a sphingosine kinase 1 specific small-molecule inhibitor.

Authors: Hengst JA, Wang X, Sk UH, Sharma AK, Amin S, Yun JK.

Abstract: The sphingolipid metabolic pathway represents a potential source of new therapeutic targets for numerous hyperproliferative/inflammatory diseases. Targets such as the sphingosine kinases (SphKs) have been extensively studied and numerous strategies have been employed to develop inhibitors against these enzymes. Herein, we report on the optimization of our novel small-molecule inhibitor SKI-I (N'-[(2-hydroxy-1-naphthyl)methylene]-3-(2-naphthyl)-1H-pyrazole-5-carbohydrazide) and the identification of a SphK1-specific analog, SKI-178, that is active in vitro and in vivo. This SphK1 specific small-molecule, non-lipid like, inhibitor will be of use to elucidate the roles of SphK1 and SphK2 in the development/progression of hyperproliferative and/or inflammatory diseases.

CiteXplore: 21050755

DOI: 10.1016/j.bmcl.2010.10.005

Patent ID: