t-Boc-aminooxy-PEG4-propargyl is a click chemistry tool containing a propargyl group and t-Boc-aminooxy group. Propargyl group is reactive with azide-bearing compounds or biomolecules via copper catalyzed Click Chemistry to yield a stable triazole linkage. T-Boc-aminooxy can be deprotected under mild acidic conditions and then can react with an aldehyde or ketone group to form a linkage. The hydrophilic PEG spacer increases solubility in aqueous media.