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

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)

Contributors

Inventor Institute
Ian Waddell Cancer Research UK Manchester Institute
Cat. #: 160405
Tool sub type: Inhibitor
Research Fields: Cancer;Cell signaling and signal transduction;Drug development
Purpose: Inhibitor
Alternate name: G6PD; G6PD1; Glucose-6-phosphate 1-dehydrogenase; glucose-6-phosphate dehydrogenase; glucose-6-phosphate dehydrogenase, glucose 6 phosphate dehydrogenase
Product 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.
Additional notes: Relevant Indications: Larynx cancer, Gastric cancer
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
Shipping conditions: Dry Ice
Solubility: 30-100M in PBS
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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