KB05yne is a site-selective, alkyne-functionalized electrophilic "probe" fragment probe designed for covalent ligand discovery, with preferential reactivity toward specific cysteine residues in proteins. KB05yne strongly labels wild-type target proteins (e.g., CDKN2AIP, HPCAL1 ) but does not label their cysteine-to-alanine mutants, confirming site-specific cysteine reactivity. KB05yne can be used for the discovery and optimization of site-specific covalent ligands, and is applicable to proteins with diverse structures and functions, especially in studies targeting cysteine residues in cancer-related or difficult-to-purify proteins [1].
In Vitro, KB05yne exhibits preferential reactivity toward specific cysteine residues in proteins, and strongly labels wild-type target proteins (e.g., CDKN2AIP, HPCAL1)[1].
References:
[1]. Crowley VM, et al. Functionalized Scout Fragments for Site-Specific Covalent Ligand Discovery and Optimization. ACS Cent Sci. 2021;7(4):613-623.
In Vitro, KB05yne exhibits preferential reactivity toward specific cysteine residues in proteins, and strongly labels wild-type target proteins (e.g., CDKN2AIP, HPCAL1)[1].
References:
[1]. Crowley VM, et al. Functionalized Scout Fragments for Site-Specific Covalent Ligand Discovery and Optimization. ACS Cent Sci. 2021;7(4):613-623.