Biotin-PEG4-Picolyl azide is a biotin reagent which can be conjugated with alkyne-containing biomolecules. This biotin reagent incorporates a copper-chelating motif that dramatically accelerates the Cu(I)-catalyzed Click Chemistry. The use of Biotin Picolyl Azide instead of conventional Biotin Azide allows for at least a tenfold reduction in the concentration of the copper catalyst without sacrificing the efficiency of labeling. The hydrophilic spacer arm provides better solubility to the labeled molecules in aqueous media.