Gypsophila paniculata is an ornamental crop with medicinal value. To date, limited information has been reported about the natural products in G. paniculata to explain its medicinal function. The current study reports the natural products found in G. paniculata stem for the first time. Thirty-three compounds were isolated from the extract of G. paniculata stem and identified by gas chromatography-mass spectrometry, 10 of which have contents >2%. These were 2-O-methyl-D-mannopyranose (37.4706%), glycerol (12.5669%), two tetratetracontane isomer (7.6523 + 3.5145%), tetrahygro-4-pyranol (5.3254%), 1,6-anhydro-beta-d-glucopyranos (4.7507%), palmitic acid (4.1848%), 4-hydroxy-3-methoxystyrene (3.7439%), methyl-octadeca-9,12-dienoate (2.7490%), and 2-deoxy-D-galactose (2.6193%). Another bioactive compound, condrillasterol, was identified with 1.3384% content. We also reported that G. paniculata possesses antioxidant activity possibly associated with the presence of a phenolic chemical 4-hydroxy-3-methoxystyrene. Our data collectively demonstrate that G. paniculata contains some bioactive compounds with high contents and antioxidants, consistent with its role as a medicinal herb.