磷酸甘油酸脱氢酶(PHGDH)的负变构调节剂(IC50 = 34.8μM)。在体外过表达PHGDH的乳腺癌细胞系中表现出抗肿瘤活性(MDA-MB-468和HCC-70细胞的EC50值分别为7.7和10.8μM)。抑制MDA-MB-468异种移植物在小鼠中的生长。
PKUMDL-WQ-2101 is a potent and selective non-NAD+-competing allosteric inhibitor of phosphoglycerate dehydrogenase (PHGDH) that selectively inhibits serine synthesis in cancer cells. PKUMDL-WQ-2101 binds to allosteric site I, which is located close to active site. PKUMDL-WQ-2101 inhibits tumor growth of MDA-MB-468 xenografts in mice.