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Glucose-6-phosphate Dehydrogenase inhibitor G6PD Small Molecule (Tool Compound)

Invented by Dr Ian Waddell
Invented at Cancer Research UK Manchester Institute

Info

Synonyms Synonyms for Glucose-6-phosphate Dehydrogenase: G6PD; G6PD1; Glucose-6-phosphate 1-dehydrogenase; glucose-6-phosphate dehydrogenase; glucose-6-phosphate dehydrogenase, glucose 6 phosphate dehydrogenase
Type Inhibitor
Relevance A selective inhibitor of Glucose-6-phosphate dehydrogenase (G6PD) which demonstrates anti-cancer activity. G6PD is a critical metabolic enzyme involved in the oxidative phase of the pentose phosphate pathway. Chinese hamster ovary cells that are devoid of G6PD display increased sensitivity to radiation and human fibroblasts deficient in G6PD display increased ROS and radiation sensitivity.
Clinically, evidence from studies in larynx and gastric cancer suggests that tumours show increased G6PD activity, and this correlates to a poor clinical outcome.
On Target IC50 1.0 µM
Selectivity Inhibitory activity against related targets as % inhibition at given concentration:

6PGDH: 4.7% at 200 µM
IDH: 0.9% at 200 µM
RET: 4.8% at 100 µM
LSD1: 6.3% at 40 µM
Key Attributes Molecular Weight: 360.5 kDa

Cell Permeability: Caco2 Permeability: 31.6 x 10-6 cm/s (efflux ratio 0.54)

Relevant Signalling Pathways: Pentose phosphate pathway (PPP)
Solubility 30-100µM in PBS
Research Area Cancer, Metabolism
Notes Relevant Indications: Larynx cancer, Gastric cancer

References

There are 2 reference entries for this reagent.

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References: 2 entries

Hamilton et al. 2012. J Med Chem. 55(9):4431-45. PMID: 22506561.

Hitchin et al. 2012. Tetrahedron Letters. 53:2868-72


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References: 2 entries

Hamilton et al. 2012. J Med Chem. 55(9):4431-45. PMID: 22506561.

Hitchin et al. 2012. Tetrahedron Letters. 53:2868-72


Add a reference

Inventor Information