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Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. Isoprenylcysteine carboxyl methyltransferase (Icmt) catalyzes the methylation of C-terminal prenylcysteine residues, the last step in this process. CAY10677 is an analog of the Icmt inhibitor cysmethynil that was developed for improved solubility and cell permeability. CAY10677 inhibits Icmt with an IC50 value of 0.86 μM and demonstrates nearly 10-fold more potent antiproliferative activity than cysmethynil on human breast cancer MDA-MB-231 cells (IC50s = 2.63 versus 27.4 μM, respectively) and human prostate cancer PC3 cells (IC50s = 2.55 versus 25.2 μM, respectively).

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