A potent and reversible inhibitor of ceramide kinase
NVP 231 is a potent, reversible and specific inhibitor of ceramide kinase(CerK) with the IC50 value of 12±2nM in radio assay [1].
NVP 231 has been noted to inhibit CerK with the IC50 value of 12±2nM and have the 90% inhibition at 100 nM in the radio assay. In addition, NVP 231 has been reported to compete with ceramide with the Ki value of 7.4 nM. Furthermore, NVP 231 has been revealed to achieve complete inhibition of CIP at 100nM. NVP 231 in an assay based on human CerK-overexpressing COS-cells (COS-CerK). And the study has been exhibited that NVP 231 is a more potent inhibitor of mouse CerK. Apart from these, NVP 231 has been shown the specificity to CerK with the IC50 values of 0.01 μM, 100 μM, >100 μM, 5 μM, >25 μM, >25 μM, >10 μM, >10 μM and >10 μM for hCerK, hSphK1, hSphK2, hDAGKα, hPI3Kα, hVps34, hGCS, hSMS-1 and CERT, respectively [1].
参考文献:
[1]Graf C1, Klumpp M, Habig M, Rovina P, Billich A, Baumruker T, Oberhauser B, Bornancin F. Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor. Mol Pharmacol. 2008 Oct;74(4):925-32.
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