Antisense oligonucleotides are highly effective equipment to regulate gene expression innovel cells and model organisms. However, a transfection or microinjection is usually needed for effective delivery with the antisense agent. We report the conjugation of a number of HIV TAT fairly peptides to a hairpin-protected antisense agent by means of a light-cleavable nucleobase caging group. This conjugation allows for the facile delivery in the antisense agent with no transfection reagent, and photochemical activation offers precise manage in excess of gene expression. The created strategy is extremely modular, as demonstrated by the conjugation of folic acid towards the caged antisense agent. This enabled targeted cell delivery by way of cell-surface folate receptors followed by photochemical triggering of antisense activity. Importantly, the presented approach delivers native oligonucleotides after light-activation, devoid p97 of any delivery functionalities or modifications that might otherwise impair their antisense exercise.