Cytokinins are phytohormones that play multiple roles to control plant growth and development. In this study, leaf biomass and the production of andrographolide compounds in a medicinal plant Andrographis paniculata were significantly increased after exogenously treating with the synthetic cytokinin cytokinin-1-(2-chloro-4-pyridyl)-3-phenylurea (CPPU) at 0 (water), 5, or 10mgL-1 and observed the results for 24h, 48h, and 7days of treatment. It was found that CPPU could significantly enhance new axillary bud formation and further promote branching 4.6-5.6-fold higher, resulting in higher fresh weight (FW) and dry weight (DW) than the control. Application of CPPU at 5mgL-1 significantly promoted the highest contents of total reducing sugar at 2.5-fold in leaves and at 1.5-fold in roots. Although treatments of CPPU significantly affected the increasing contents of chlorophyll and carotenoid (1.2-1.6-fold), CPPU at 10mgL-1 slightly caused leaf stress and chlorophyll reduction. Interestingly, 5mgL-1 CPPU could enhance andrographolide content, an active anti-infectious compound in Andrographis paniculata (2.2-fold higher than the control) that reached the highest content at 24h after treatment. This study suggested that CPPU should be suitable for field application to promote leaf yields and induce the production of useful pharmaceutical compounds in Andrographis paniculata.