1. Metabolic Enzyme/Protease
  2. Phosphoglycerate Dehydrogenase (PHGDH)
  3. PKUMDL-WQ-2201

PKUMDL-WQ-2201 

Cat. No.: HY-123418
Handling Instructions

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.

For research use only. We do not sell to patients.

PKUMDL-WQ-2201 Chemical Structure

PKUMDL-WQ-2201 Chemical Structure

CAS No. : 592474-91-4

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Description

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].

IC50 & Target

IC50: 35.7 μM (PHGDH WT), 69 μM (PHGDH T59A), >300 μM (PHGDH T56AK57A)[1]

In Vitro

PKUMDL-WQ-2201 (10 nM-100 μM; 3 d) shows good selectivity for PHGDH-amplified breast cancer cell lines, inhibits cell viability with EC50s of 7.7 μM (MDA-MB-468) and 10.8 μM (HCC70), respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PKUMDL-WQ-2201 (5-20 mg/kg; i.p.; once daily for 30 d) exhibits substantial inhibitory effects on MDA-MB-468 xenografts compared with vehicle-treated mice, without affecting the tumor growth[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

351.81

Formula

C15H14ClN3O3S

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PKUMDL-WQ-2201
Cat. No.:
HY-123418
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