Chemical Name:4-[[4-(4-Chlorophenyl)-2-thiazolyl]amino]phenol
Biological Activity:
Selective non-lipid inhibitor of sphingosine kinase (IC50
= 0.5 μM); does not act at
ATP-binding site. Displays no inhibition of ERK2, PI 3-kinase, or PKCα at concentrations up to 60 μM. Reduces levels of sphingosine-1-phosphate in MDA-MB-231
breast cancer cells. Induces apoptosis and inhibits proliferation in several
other tumour cell lines in vitro (IC50 = 0.9-4.6 μM).
Frenchet al (2003) Discovery and evaluation of inhibitors of
human sphingosine kinase. Cancer Res. 63 5862. Frenchet
al (2006) Antitumor activity of sphingosine kinase inhibitors.
J.Pharmacol.Exp.Ther. 318 596.
