Photocaging facilitates non-invasive and precise spatio-temporal control over the release of biologically relevant small-and macro-molecules using light. However,s ubcellular organelles are dispersed in cells in am anner that renders selective light-irradiation of ac omplete organelle impractical. Organelle-specific photocages could provide ap owerfulm ethod for releasing bioactive molecules in subcellular locations.H erein, we report ag eneral post-synthetic method for the chemical functionalization and further conjugation of meso-methyl BODIPY photocages and the synthesis of endoplasmic reticulum (ER)-, lysosome-, and mitochondria-targeted derivatives.W ea lso demonstrate that 2,4dinitrophenol, am itochondrial uncoupler,a nd puromycin, ap rotein biosynthesis inhibitor,c an be selectively photoreleased in mitochondria and ER, respectively,i nl ive cells by using visible light. Additionally,p hotocaging is shown to lead to higher efficacy of the released molecules,probably owingto alocalized and abrupt release.Supportinginformation and the ORCID identification number(s) for the author(s) of this article can be found under: https://doi.org/10.