CAY10677

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.¹ 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).¹

1. Ramanujulu, P.M., Yang, T., Yap, S.Q., et al. Functionalized indoleamines as potent, drug-like inhibitors of isoprenylcysteine carboxyl methyltransferase (Icmt) Eur. J. Med. Chem. 63,378-386(2013).