The incorporation of a labeled 13C atom provides a plethora of opportunities in organic synthesis and catalysis. Structure of complicated compounds can be successfully confirmed using the precise location of a labeled carbon atom; a reaction mechanism can be supported by the presence or absence of a label in reaction products; metabolic pathways of biological compounds can be found out depending on labeled products; the concentration of analyzed labeled compounds can be significantly lower for recording and successful interpretation of NMR spectra, etc. This review aims to provide a researcher with common and promising strategies for the synthesis of labeled compounds so that a researcher can select an appropriate route to save valuable labeled material. All the labeling approaches were considered based on starting labeling source. Ideological aim of the review is to demonstrate the opportunities for label incorporation so that a researcher can find the improvements in his own topic using labeled compounds. Utilization of labeled compounds in catalysis and studying reaction mechanisms were also considered to demonstrate the capabilities of labeled compounds, which may be useful in specific tasks and applications. The potential of labeled compounds in bioactive compound metabolite analysis was demonstrated on selected examples.