Glucose-6-phosphate Dehydrogenase inhibitor G6PD Small Molecule (Tool Compound)
- Name Ian Waddell
- Institute Cancer Research UK Manchester Institute
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
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
- • Hamilton et al. 2012. J Med Chem. 55(9):4431-45. PMID: 22506561.
- • Hitchin et al. 2012. Tetrahedron Letters. 53:2868-72