PKUMDL-WQ-2201 is a PHGDH non-NAD+-competing allosteric inhibitor ( IC 50 =35.7 μM). PKUMDL-WQ-2201 also inhibits PHGDH mutants with IC 50 s of 69 μM (T59A) and >300 μM (T56AK57A), respectively. PKUMDL-WQ-2201 inhibits de novo serine synthesis in cancer cells, and reduces tumor growth.
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