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Targeting Ceramide Metabolism With a Potent and Specific Ceramide Kinase Inhibitor

Targeting Ceramide Metabolism With a Potent and Specific Ceramide Kinase Inhibitor

Christine Graf, Martin Klumpp, Michael Habig, Philipp Rovina, Andreas Billich, Thomas Baumruker, Berndt Oberhauser, Frédéric Bornancin

Mol Pharmacol. 2008 Oct;74(4):925-32.

PMID: 18612076

Abstract:

Ceramide kinase (CerK) produces the bioactive lipid ceramide-1-phosphate (C1P) and appears as a key enzyme for controlling ceramide levels. In this study, we discovered and characterized adamantane-1-carboxylic acid (2-benzoylamino-benzothiazol-6-yl)amide (NVP-231), a potent, specific, and reversible CerK inhibitor that competitively inhibits binding of ceramide to CerK. NVP-231 is active in the low nanomolar range on purified as well as cellular CerK and abrogates phosphorylation of ceramide, resulting in decreased endogenous C1P levels. When combined with another ceramide metabolizing inhibitor, such as tamoxifen, NVP-231 synergistically increased ceramide levels and reduced cell growth. Therefore, NVP-231 represents a novel and promising compound for controlling ceramide metabolism that may provide insight into CerK physiological function.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP362003836	NVP-231		362003-83-6	Price

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