AMP-activated protein kinase (AMPK) is a critical energy sensor, consisting of α, β, and γ subunits, forming a heterotrimeric complex. It is widely distributed in various cells and regulates energy balance by sensing the AMP/ATP ratio within the cell. AMPK is involved in the regulation of glucose metabolism, fatty acidoxidation, and cell growth. Activation of AMPK promotes energy production pathways while inhibiting energy-consuming processes to maintain cellular energy stability. Its expression shows specificity in different tissues, and its activation state or gene mutations are closely associated with various diseases such as diabetes, obesity, cardiovascular diseases, and cancer. Specific activation of AMPK is considered a potential strategy for treating metabolic disorders and related diseases.