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In search of suitable tool to target the endoplasmic reticulum of human tumor cells, a non-cytotoxic aza-BODIPY derivative was designed and accessed in a simple synthesis in a few steps from commercially available starting materials. This aza-BODIPY was conjugated to 3-O-acetyl-triterpene carboxylic acids (glycyrrhetinic, ursolic, oleanolic, and betulinic acid) using a piperazinyl spacer. The resulting conjugates exhibited no cytotoxicity but were able to selectively target the ER.