WQ-2101

WQ-2101 is a potent and selective small molecule inhibitor of phosphoglycerate dehydrogenase (PHGDH), the rate-limiting enzyme in the serine synthesis pathway (SSP). PHGDH catalyzes the conversion of 3-phosphoglycerate to 3-phosphohydroxypyruvate, a critical step for the production of serine and downstream nucleotides required for rapid cell proliferation. WQ-2101 is primarily utilized as a chemical probe in preclinical research to investigate metabolic reprogramming in cancer. Studies have demonstrated that WQ-2101 exerts anti-leukemic effects in acute myeloid leukemia (AML) models, particularly those resistant to PI3K/mTOR inhibition, by inducing apoptosis and increasing mitochondrial reactive oxygen species (ROS) levels. It is often studied alongside other PHGDH inhibitors like NCT-503 to explore therapeutic strategies for cancers that overexpress the serine synthesis pathway.