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NVP-231 is a potent and reversible inhibitor of ceramide kinase (IC50 = 12 nM).1 It is selective for ceramide kinase over SPHK1, SPHK2, DAGKa, PI3Ka, PI4Kb, VPS34, GCS, SMS-1, and CERT (IC50s = >5 mM). NVP-231 inhibits formation of ceramide-1-phosphate (C1P; IC50 = 10 nM) and cell death in ceramide kinase overexpressing COS cells (COS-CerK). It also inhibits C1P formation and tube formation in murine dermal microvascular endothelial cells when used at a concentration of 100 nM.2
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1. Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor. Mol. Pharm. 74(4), 925-932 (2008).
2. Ceramide kinase deficiency impairs microendothelial cell angiogenesis in vitro. Microvasc. Res. 77(3), 389-393 (2009).