Chemical Structure : WQ-2101
CAS No.: 304481-72-9
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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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.
M.Wt | 317.257 | |
Formula | C14H11N3O6 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
2,4-Dihydroxy-N'-(2-hydroxy-5-nitrobenzylidene)benzohydrazide |
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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