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WQ-2101

Chemical Structure : WQ-2101

CAS No.: 304481-72-9

WQ-2101 (WQ2101;WQ 2101;PKUMDL-WQ-2101)

Catalog No.: PC-35907Not For Human Use, Lab Use Only.

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).

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Biological Activity

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).
WQ-2101 binds to allosteric site I, inhibits the serine biosynthesis pathway in cells.
WQ-2101 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).
WQ-2101 selectively inhibit de novo serine synthesis in cancer cells, and reduce tumor growth in vivo.

Physicochemical Properties

M.Wt 317.257
Formula C14H11N3O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2,4-Dihydroxy-N'-(2-hydroxy-5-nitrobenzylidene)benzohydrazide

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.

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