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NVP-231 is a potent, selective, and reversible small molecule inhibitor of ceramide kinase (CERK). Developed by Novartis, it competitively inhibits the binding of ceramide to CERK with low-nanomolar potency (IC50 of 12 nM), thereby blocking the phosphorylation of ceramide to ceramide-1-phosphate (C1P). By disrupting ceramide homeostasis, NVP-231 shifts sphingolipid metabolism toward ceramide accumulation, which can induce cell cycle arrest (specifically in the M phase) and trigger apoptosis. It is widely utilized as a chemical probe in research investigating sphingolipid signaling, cell proliferation, inflammation, and endocrine therapy-resistant breast cancer.
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