GSA-10 is a novel, potent activator of the smoothened receptor (Smo). GSA-10 binds to Smo at a unique site compared to agonists such as SAG and purmorphamine, and is not affected by the Smo antagonist cyclopamine. GSA-10 promotes the differentiation of mesenchymal pluripotent C3H10T1/2 cells into osteoblasts.