KB05yne

KB05yne is a site-selective, alkyne-functionalized electrophilic "scout" fragment probe designed for covalent ligand discovery, with preferential reactivity toward specific cysteine residues in proteins. KB05yne strongly labels wild-type forms of target proteins (e.g., CDKN2AIP, HPCAL1) but not their cysteine-to-alanine mutants, confirming site-specific cysteine reactivity. KB05yne can be used for site-specific covalent ligand discovery and optimization for structurally and functionally diverse proteins, particularly in studies targeting cysteine residues in cancer-related or difficult-to-purify proteins[1].