The efficiency of a copper (Cu(I))-catalyzed Azide-Alkyne click chemistry reaction (CuAAC) strongly depends on the presence of copper ions Cu(+I). Copper(I) ions are easily oxidized and undergo disproportionation, also has cytotoxic effects to living cell. Tertiary amine and triazine bearing ligands ligands can stabilize Cu(I) and accelerate the reaction. These ligands further expand the CuAAC applications in chemical biology because of biorthogonality, low cytotoxic, and reaction rate.