304481-72-9

PKUMDL-WQ-2101 is a non-NAD+-competing allosteric phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 34.8 μM. PKUMDL-WQ-2101 exhibits antitumor activity[1].

PKUMDL-WQ-2101 is a potent and selective non-NAD+-competing allosteric inhibitor of phosphoglycerate dehydrogenase (PHGDH) th at selectively inhibits serine synthesis in cancer cells. PKUMDL-WQ-2101 binds to allosteric site Iwhich is located close to active site. PKUMDL-WQ-2101 inhibits tumor growth of MDA-MB-468 xenografts in mice.

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[1] Qian Wang, et al. Rational Design of Selective Allosteric Inhibitors of PHGDH and Serine Synthesis with Anti-tumor Activity. Cell Chem Biol. 2017 Jan 19;24(1):55-65. DOI:10.1016/j.chembiol.2016.11.013