cysmethynil

Cysmethynil is a potent, small-molecule inhibitor of isoprenylcysteine carboxylmethyltransferase (ICMT), an enzyme that catalyzes the post-translational carboxylmethylation of C-terminal prenylated proteins, such as Ras and other small GTPases. This modification is critical for the proper membrane localization and biological activity of these proteins. By blocking ICMT, Cysmethynil disrupts oncogenic signaling pathways, leading to cell cycle arrest and apoptosis. Research, particularly from Duke-NUS Medical School, has demonstrated its efficacy in preclinical models of pancreatic, prostate, and liver cancers, where it induces mitochondrial dysfunction and energy depletion.