Organelle-localizable small-molecule ligands are valuable tools for spatiotemporally controlling protein localization and signaling processes in living cells. Here, we present synthetic ligands that specifically localize to the Golgi surface. The ligands can rapidly recruit their target proteins from the cytoplasm to the Golgi and be applied to manipulate signaling proteins and lipids on the Golgi membrane, offering a new useful chemical tool for the study and control of Golgi/cell functions.