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V-11-0711 is a potent and selective small-molecule inhibitor of choline kinase alpha (ChoKα) with an IC50 of 20 nM. Developed by Vertex Pharmaceuticals, V-11-0711 binds to the active site of ChoKα, inhibiting its catalytic activity and reducing phosphocholine (PCho) levels without affecting the protein levels of the enzyme. It has been utilized as a preclinical chemical probe to investigate the role of ChoKα in cancer cell survival, particularly in breast cancer (including triple-negative breast cancer) and cervical cancer. Preclinical studies demonstrate that V-11-0711 causes reversible growth arrest rather than apoptosis at lower concentrations, suggesting that the non-catalytic scaffolding function of ChoKα, rather than its catalytic activity alone, may be critical for cancer cell survival.
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