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Glucose-6-phosphate Dehydrogenase inhibitor G6PD Small Molecule (Collaborative Toolkit)

Invented by Dr Ian Waddell

Info

Antigen/Gene or Protein Targets Glucose-6-phosphate dehydrogenase (G6PD)
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.

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
Modulatory Function Inhibitor
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
Solubility and Solvent 30-100µM in PBS
Molecular Weight (kDa) 360.5
Cell Permeability Caco2 Permeability: 31.6 x 10-6 cm/s (efflux ratio 0.54)
Research Area Cancer, Metabolism
Relevant Indications Larynx cancer, Gastric cancer
Relevant Signalling Pathways Pentose phosphate pathway (PPP)
Negative Control Available Yes
Negative Control Information Structurally related negative control available

IC50 (G6PD): >200 µM

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