Since PGK1 is the key glycolytic enzyme in the glycolytic process, we evaluated the metabolic profile in glioma cells after P7C3 treatment and we demonstrated that P7C3 indeed significantly suppressed the aerobic glycolysis in glioma cells, which was manifested as a declining extracellular acidification rate (ECAR), as well as significantly decreasing the intracellular levels of lactate, pyruvate, and ATP. This evidence concerns the gene HK1 and central nervous system cancer.