This review evaluates the emerging roles of SRT2104, a potent small molecule activator of Silent Information Regulator 1 (SIRT1), in disease treatment. SIRT1, a NAD+-dependent deacetylase, plays crucial roles in various cellular processes and is implicated in numerous diseases. SRT2104, identified through high-throughput screening, has shown superior binding affinity and stability compared to other SIRT1 activators. Preclinical and clinical studies have demonstrated its therapeutic potential in conditions such as neurodegenerative diseases (Alzheimer's, Parkinson's, Huntington's), brain ischemia/reperfusion injury, depression, diabetic complications, lipid metabolism disorders, musculoskeletal diseases, and chronic obstructive pulmonary disease (COPD). SRT2104 has been found to modulate SIRT1 activity, which in turn affects various pathways and molecular targets, leading to improved outcomes in these diseases. The review highlights the promising therapeutic potential of SRT2104, supported by its favorable pharmacokinetics, safety profile, and molecular mechanisms of action.This review evaluates the emerging roles of SRT2104, a potent small molecule activator of Silent Information Regulator 1 (SIRT1), in disease treatment. SIRT1, a NAD+-dependent deacetylase, plays crucial roles in various cellular processes and is implicated in numerous diseases. SRT2104, identified through high-throughput screening, has shown superior binding affinity and stability compared to other SIRT1 activators. Preclinical and clinical studies have demonstrated its therapeutic potential in conditions such as neurodegenerative diseases (Alzheimer's, Parkinson's, Huntington's), brain ischemia/reperfusion injury, depression, diabetic complications, lipid metabolism disorders, musculoskeletal diseases, and chronic obstructive pulmonary disease (COPD). SRT2104 has been found to modulate SIRT1 activity, which in turn affects various pathways and molecular targets, leading to improved outcomes in these diseases. The review highlights the promising therapeutic potential of SRT2104, supported by its favorable pharmacokinetics, safety profile, and molecular mechanisms of action.