PKUMDL-WQ-2201

PKUMDL-WQ-2201 is a PHGDH non-NAD+-competing allosteric inhibitor (IC50=35.7 μM) . PKUMDL-WQ-2201 also inhibits PHGDH mutants with IC50s of 69 μM (T59A) and >300 μM (T56AK57A), respectively. PKUMDL-WQ-2201 inhibits de novo serine synthesis in cancer cells, and reduces tumor growth[1][2].

Product Specifications

CAS Number

[592474-91-4]

UNSPSC

12352005

Target

Phosphoglycerate Dehydrogenase (PHGDH)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pkumdl-wq-2201.html

Purity

98.45

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(C=C1Cl)C2=CC=C(O2)/C=N/NC(NCC)=S)O

Molecular Formula

C15H14ClN3O3S

Molecular Weight

351.81

References & Citations

[1]Zhao JY, et al. A retrospective overview of PHGDH and its inhibitors for regulating cancer metabolism. Eur J Med Chem. 2021 May 5;217:113379. |[2]Wang Q, 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.