2. Metabolic Enzyme/Protease
  3. Phosphoglycerate Dehydrogenase (PHGDH)
  4. PKUMDL-WQ-2101

PKUMDL-WQ-2101 is a non-NAD+-competing allosteric phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 34.8 μM. PKUMDL-WQ-2101 exhibits antitumor activity.

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

PKUMDL-WQ-2101 Chemical Structure

PKUMDL-WQ-2101 Chemical Structure

CAS No. : 304481-72-9

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Based on 1 publication(s) in Google Scholar

PKUMDL-WQ-2101 Related Antibodies

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Description

PKUMDL-WQ-2101 is a non-NAD+-competing allosteric phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 34.8 μM. PKUMDL-WQ-2101 exhibits antitumor activity[1].

IC50 & Target

IC50: 34.8 μM (PHGDH)[1]
In Vitro

PKUMDL-WQ-2101 (72 hours) shows dose-dependent suppression effects on the cell viability at micromolar concentrations, with good selectivity for PHGDH amplified breast cancer cell lines. The antitumor activities of PKUMDL-WQ-2101 in the two PHGDH amplified breast cancer cell lines (MDA-MB-468 and HCC70) are 7.70 μM and 10.8 μM, respectively[1].
PKUMDL-WQ-2101 (2.5-40 μM; 24 hours) causes cell cycle arrest in MDA-MB-468 cells[1].
PKUMDL-WQ-2101 (37 μM; 24 hours) decreases de novo serine synthesis and metabolism downstream of the serine synthesis pathway, with effects comparable to PHGDH genetic deletion[1].

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

PKUMDL-WQ-2101 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 2.5 μM, 5.0 μM, 20 μM and 40 μM
Incubation Time: 24 hours
Result: Caused cell cycle arrest.
In Vivo

PKUMDL-WQ-2101 (5-20 mg/kg; i.p; daily; for 30 days) exhibits substantial inhibitory effects on MDA-MB-468 xenografts[1].

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

Animal Model: NOD.CB17 Scid/J mice injected with MDA-MB-468 cells[1]
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: i.p; daily; for 30 days
Result: Exhibited substantial inhibitory effects on MDA-MB-468 xenografts.
Molecular Weight

317.25

Formula

C14H11N3O6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(C=C1O)O)N/N=C/C2=CC([N+]([O-])=O)=CC=C2O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (394.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1521 mL 15.7604 mL 31.5209 mL
5 mM 0.6304 mL 3.1521 mL 6.3042 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1521 mL 15.7604 mL 31.5209 mL 78.8022 mL
5 mM 0.6304 mL 3.1521 mL 6.3042 mL 15.7604 mL
10 mM 0.3152 mL 1.5760 mL 3.1521 mL 7.8802 mL
15 mM 0.2101 mL 1.0507 mL 2.1014 mL 5.2535 mL
20 mM 0.1576 mL 0.7880 mL 1.5760 mL 3.9401 mL
25 mM 0.1261 mL 0.6304 mL 1.2608 mL 3.1521 mL
30 mM 0.1051 mL 0.5253 mL 1.0507 mL 2.6267 mL
40 mM 0.0788 mL 0.3940 mL 0.7880 mL 1.9701 mL
50 mM 0.0630 mL 0.3152 mL 0.6304 mL 1.5760 mL
60 mM 0.0525 mL 0.2627 mL 0.5253 mL 1.3134 mL
80 mM 0.0394 mL 0.1970 mL 0.3940 mL 0.9850 mL
100 mM 0.0315 mL 0.1576 mL 0.3152 mL 0.7880 mL
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PKUMDL-WQ-2101 Related Classifications

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.

Keywords:

PKUMDL-WQ-2101304481-72-9Phosphoglycerate Dehydrogenase (PHGDH)de novo serine synthesisPHGDHantitumor activitycell cycle arrestInhibitorinhibitorinhibit

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