Used primarily as a highly selective covalent inhibitor in chemical biology and medicinal chemistry research. Its main application lies in the development of targeted covalent inhibitors (TCIs), where the sulfonyl fluoride group reacts selectively with nucleophilic amino acid residues—particularly lysine and tyrosine—in proteins. The bromine atom enables further functionalization via cross-coupling reactions such as Suzuki or Heck reactions, allowing modular derivatization for structure-activity relationship (SAR) studies.

Commonly employed as a key intermediate in the synthesis of sulfonyl fluoride-based probes for activity-based protein profiling (ABPP), helping identify and characterize enzyme function in complex biological systems. Due to its enhanced stability and reactivity profile compared to other sulfonyl halides, it is favored in the design of chemical probes and covalent drugs targeting specific disease-related proteins. Also used in fragment-based drug discovery (FBDD) platforms where it serves as an electrophilic fragment to screen protein interactions.