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Realising the enormous potential of stem cells for regenerative medicine and drug discovery is one of the next major challenges in science. Before stem cell technology can be fully realised, obstacles remain to be overcome, including the development of cost-effective, efficient and scalable culture methods. Stem cells are capable of dividing perpetually and differentiating to all tissue types in the adult body, such as bone, muscle, nerves and all organs. The transformation of a stem cell to a fully differentiated cell within adult tissue occurs via a number of steps controlled by a combination of cellular events. The use of small molecules to control the destiny of stem cells in vitro and in vivo is an emerging discipline which offers unprecedented advantages over other techniques in terms of speed, cost, reproducibility and the ability to influence stem cell fate reversibly. This chapter summarizes the current state of the art of small molecule manipulation of stem cells and outlines how these discoveries can revolutionise drug discovery.

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