A novel bioactive macromolecule based on morpholino-functionalized phosphorus dendrimers (generation 2, G2-Mor+) was developed for osteogenic differentiation of mesenchymal stem cells (MSCs). Interestingly, through in vitro tests, it was shown that G2-Mor+ dendrimer can strongly promote the transformation of MSCs into osteoblasts, which implies the potential application of phosphorus dendrimers in bone regeneration for precision regenerative medicine.