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 10 mg L-1 and observed the results for 24 h, 48 h, and 7 days 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 5 mg L-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 10 mg L-1 slightly caused leaf stress and chlorophyll reduction. Interestingly, 5 mg L-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 24 h 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.