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PKUMDL WQ 2101

Names

[ CAS No. ]:
304481-72-9

[ Name ]:
PKUMDL WQ 2101

[Synonym ]:
Benzoic acid, 2,4-dihydroxy-, 2-[(1E)-(2-hydroxy-5-nitrophenyl)methylene]hydrazide
MFCD00589939
2,4-Dihydroxy-N'-[(E)-(2-hydroxy-5-nitrophenyl)methylene]benzohydrazide

Biological Activity

[Description]:

WQ-2101 (WQ2101, PKUMDL-WQ-2101) is a specific, allosteric inhibitor of PHGDH with IC50 of 34.8 uM (WT PHGDH), shows dramatically reduced potenecy for mutants R134A (IC50 =141 uM) and K57AT59A (IC50=128 uM); shows dose-dependent suppression effects on the cell viability at micromolar concentrations, with good selectivity for PHGDH amplified breast cancer cell lines (MDA-MB-468 and HCC70 IC50= 7.70 and 10.8 uM); selectively inhibit de novo serine synthesis in cancer cells, and reduce tumor growth in vivo.

[References]

References 1. Reid MA, et al. Nat Commun. 2018 Dec 21;9(1):5442. 2. Wang Q, et al. Cell Chem Biol. 2017 Jan 19;24(1):55-65. View Related Products by Target PHGDH

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C14H11N3O6

[ Molecular Weight ]:
317.254

[ Exact Mass ]:
317.064789

[ LogP ]:
4.51

[ Index of Refraction ]:
1.677

Related Compounds

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