PKUMDL-WQ-2201 is a PHGDH non-NAD+-competing allosteric inhibitor (IC50=35.7 μM) . PKUMDL-WQ-2201 also inhibits PHGDH mutants with IC50s of 69 μM (T59A) and >300 μM (T56AK57A), respectively. PKUMDL-WQ-2201 inhibits de novo serine synthesis in cancer cells, and reduces tumor growth[1][2].