Streptomyces species have long been recognized as prolific producers of bioactive compounds with therapeutic potential. In this study, our focus rested on the isolation and identification of Streptomyces griseorubens (AUMC B-519) among a diverse collection of 94 different actinomycete isolates obtained from several soil sites across Egypt. Our exploration was performed through the assessment of pigment production among these isolates. To gain deeper insights into the chemical composition of S. griseorubens; we employed metabolomic profiling using gas chromatography-mass spectrometry (GC-MS) and ultra-performance liquid chromatography-mass spectrometry (UPLC-MS) hyphenated with quadrupole-time-of-flight tandem mass spectrometry (QTOF-MS). This comprehensive metabolomic analysis provided a detailed view of the metabolites present in the extract, allowing us to identify key compounds responsible for the observed bioactivities. The GC-MS analysis enabled the detection of 21 compounds while, the UPLC-MS afforded 44 compounds, including a wide range of secondary metabolites, such as glycosides, carboxylic acid derivatives, lipids of triterpene derivatives, alkaloids, and flavonoids. Most of the identified compounds were described for the first time from this strain. In parallel, we assessed the antioxidant and anticancer potentialities of the ethyl acetate extract. The extract revealed restrained anticancer activity against MCF7 cell line coupled with a mild effect against 1, 1- diphenyl-2-picryl hydrazyl (DPPH) scavenging, exhibiting MIC values of 343.34 and 55.97µg/mL, respectively. This study unequivocally underscores the potential of S. griseorubnes as a valuable source of bioactive compounds. Moreover, the metabolomic profiling approach revealed the intricate chemical diversity within the extract, shedding light on the complex metabolic pathways and compounds produced by this Streptomyces strain. These findings contribute to our understanding of S. griseorubens pharmacological properties and pave the way for further investigations into its biomedical applications.