NVP-231
Ceramide kinase inhibitor / Reversible inhibitor of ceramide kinase (IC50 = 12 nM).1 At 10 nM, it inhibited ceramide-1-phosphate formation by >50% and at 100 nM it completely inhibited its formation in cell culture. NVP-231 was inactive against hSphK1/2, hPI3Ka, hPI4Kb, hVps34, hGCS, hSMS-1, CERT, and 500-fold less potent against hDAGKa. NVP-231 inhibited breast and lung cancer cell proliferation via M phase arrest.2 It potently blocked cell migration and invasion in PANC-1 pancreatic cancer cells3 as well as MDA-MB-231 breast cancer cells4.
Biochemicals & reagents
362003-83-6
Graf et al. (2008), Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor; Mol. Pharmacol., 74 925 Pastukhov et al. (2014), The ceramide kinase inhibitor NVP-231 inhibits breast and lung cancer cell proliferation by inducing M phase arrest and subsequent cell death; Br. J. Pharmacol., 171 5829 Rivera et al. (2016), Ceramide-1-phosphate regulates cell migration and invasion of human pancreatic cancer cells; Biochem. Pharmacol., 102 107 Schwalm et al. (2020), Ceramide Kinase Is Upregulated in Metastatic Breast Cancer Cells and Contributes to Migration and Invasion by Activation of PI3-Kinase and Akt; Int. J. Mol. Sci., 21 1396
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TARGET: Kinase -- PATHWAY: Cell cycle; PI3K; AKT; Cell migration -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer