NVP-231 is 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.
CAS Number: 362003-83-6
Molecular Weight: 431.55
Chemical Name: N -[2-(Benzoylamino)-6-benzothiazolyl]tricyclo[220.127.116.11,7]decane-1-carboxamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
NVP-231 (0-500 nM; 24 hours) gradually reduces the cellular CerK activity, as measured by NBD-C1P formation, demonstrating that NVP-231 active in transfected cells. The IC50 for CerK in this cellular system is 59.70 ± 12 nM. NVP-231 (0-1000 nM; 48 hours) decreases cell viability as a dose-dependent manner. This compound shows IC50 values of 1 μM in MCF-7 cells and 500 nM in NCI-H358 cells. NVP-231 (1 μM; 24-72 hours) induces caspase-3 and caspase-9 cleavage in both cell lines. However, the highest caspase-3 and caspase-9 cleavage and activation occurred at 24 hours in MCF-7 cells, then decreases again. In NCI-H358 cells, caspase-3 and caspase-9 cleavage occurrs continuously over 72 hours. NVP-231 (0-500 nM; 24 hours) causes a concentration-dependent up-regulation of cyclin B1 phosphorylation at Ser133 and a reduction of CDK1 phosphorylation at Tyr15. The total CDK1 expression also declined upon CerK inhibition
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- Graf C, Rovina P, Bornancin F. A secondary assay for ceramide kinase inhibitors based on cell growth inhibition by short-chain ceramides. Anal Biochem. 2009 Jan 1;384(1):166-9. doi: 10.1016/j.ab.2008.09.008. Epub 2008 Sep 14. PubMed PMID: 18831956.
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