Antisense oligonucleotides are highly effective tools to manage gene expression indefinitely cells and model organisms. Having said that, a transfection or microinjection is commonly needed for efficient delivery on the antisense agent. We report the conjugation of various HIV TAT KU-0063794 peptides to a hairpin-protected antisense agent by means of a light-cleavable nucleobase caging group. This conjugation enables for the facile delivery in the antisense agent with no transfection reagent, and photochemical activation offers precise control more than gene expression. The formulated technique is highly modular, as demonstrated from the conjugation of folic acid to your caged antisense agent. This enabled targeted cell delivery by means of cell-surface folate receptors followed by photochemical triggering of antisense action. Importantly, the presented approach delivers native oligonucleotides right after light-activation, devoid p97 of any delivery functionalities or modifications that could otherwise impair their antisense activity.