Ceramide Kinase Inhibitor II, NVP-231

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.

Packaged under inert gas

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

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

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

Toxicity: Standard Handling (A)