Glucose-6-phosphate Dehydrogenase inhibitor G6PD Small Molecule (Tool Compound)
Invented by Dr Ian Waddell
Invented at Cancer Research UK Manchester Institute
- Datasheet
- References (2)
- Inventor Info
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: 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
Inventors
|
Dr Ian Waddell |
