Sphingosine Kinase Inhibitor

Biochem/physiol Actions

Reversible: yes

Target IC₅₀: 0.5 µM for GST-hSK

Product competes with ATP.

Primary TargetGST-hsk

Cell permeable: yes

General 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 µM for GST-hSK). Does not affect the kinase activity of hERK2, hPI3K, or PKCα even at concentrations as high as 60 µM. Induces apoptosis in human cancer cells that express the drug transport proteins Pgp or MRP1 (IC₅₀ = ~ 1-5 µM) 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 PKC_α at cocentrations as high as 60 µM. Shown to induce apoptosis in human cancer cells that express the drug transport proteins Pgp or MRP1 (IC₅₀ ~1-5 µM) by inhibiting sphingosine-1-phosphate production.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

French, K.J., et al. 2003. Cancer Res.63, 5962.

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Carcinogenic / Teratogenic (D)