General description

A cell-permeable benzothiazole compound that potently inhibits Cer (ceramide) phosphorylation by CerK (Cer Kinase) in a reversible and Cer-, but not ATP-, competitive manner (IC₅₀ = 12 nM; K_i = 7.4 nM) with excellent selectivity over hDAGKα (IC₅₀ = 5 µM) and little or no activity against eight other lipid metabolizing enzymes and kinases (IC₅₀ ≥10 µM) in cell-free enzymatic assays. When applied to live cells in cultures, NVP-231 effectively prevents the binding of Cer to CerK, making cellular Cer more available to other Cer metabolizing enzymes and resulting in an increased GlcCer (glucosylceramide) and SM (sphingomyelin) production in addition to the expected decrease of Cer phosphorylation.

Legal Information

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

Other Notes

Graf, C., et al. 2008. Mol. Pharmacol.74, 925.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)