SMALL MOLECULES
Contributor Information
- Name Ian Waddell
- Institute Cancer Research UK Manchester Institute
Tool Details
- Tool name: Glucose-6-phosphate Dehydrogenase inhibitor G6PD Small Molecule (Tool Compound)
- Alternate names: G6PD; G6PD1; Glucose-6-phosphate 1-dehydrogenase; glucose-6-phosphate dehydrogenase; glucose-6-phosphate dehydrogenase, glucose 6 phosphate dehydrogenase
- Tool type: Small molecules
- Tool sub-type: Inhibitor
- Purpose: Inhibitor
- Cancer type: Head and neck cancer; Digestive / Gastrointestinal cancer
- Description: 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.
- Research area: Cancer; Cell Signaling & Signal Transduction; Drug Discovery & Development
- Selectivity: Inhibitory activity against related targets as % inhibition at given concentration: 6PGDH: 4.7% at 200 ÂľM IDH: 0.9% at 200 ÂľM RET: 4.8% at 100 ÂľM LSD1: 6.3% at 40 ÂľM
- IC50: 1.0 ÂľM
- Additional notes: Relevant Indications: Larynx cancer, Gastric cancer
- For Research Use Only
Target Details
Application Details
Handling
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Solubility: 30-100
- Shipping conditions: Dry Ice
Documentation
Related Tools
References
- • 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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