CPO-PFP is an invaluable reagent for targeted protein modification and other versatile applications. This easy-to-handle, stable white solid is soluble in water, making it convenient to work with. Under mild conditions, the reaction with CPO-PFP yields stable derivatives of 1,4-thiazepan-5-one with excellent efficiency1. It displays remarkable selectivity for N-terminal cysteine residues, allowing modification even in the presence of internal cysteine residues on the same protein, other proteins, biological thiols, and nucleophilic reagents like DTT. Furthermore, CPO-PFP serves as a universal precursor, enabling the synthesis of CPO-primary amides2.
Synonyms: 2,3,4,5,6-pentafluorophenyl 4-(3-oxocycloprop-1-en-1-yl) butanoate; CPO-PFP
Platform for Orthogonal N -Cysteine-Specific Protein Modification Enabled by Cyclopropenone Reagents.
Istrate A.; Geeson M.; Navo C.; Sousa B.; Marques M.; Taylor R.; Journeaux T.; Oehler S.; Mortensen M.; Deery M.; Bond A.; Corzana F.; Jiménez-Osés G.; Bernardes G. J Am Chem Soc 2022, 144 (23), 10396–10406. DOI: 10.1021/jacs.2c02185
Strategies and Challenges for the next Generation of Antibody–Drug Conjugates.
Beck A.; Goetsch L.; Dumontet C.; Corvaïa N. Nat Rev Drug Discov 2017, 16 (5), 315–337. DOI: 10.1038/nrd.2016.268
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