Potent inhibitor of farnesyltransferase in isolated enzyme assays (IC50=30 nM) and in whole cells. Inhibition of farnesyltransferase is selective over geranylgeranyltransferase I and II (IC50=35.8 µM and 67 µM respectively). α-Hydroxyfarnesylphosphonic acid inhibited (1 µM) Ras processing in Ha-ras-transformed NIH 3T3 fibroblasts.
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