#152789

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

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Cat. #152789

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

Cat. #: 152789

Sub-type: Inhibitor

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Contributor

Inventor: Dr Ian Waddell

Institute: Cancer Research UK Manchester Institute

Tool Details
Handling
Target Details
Application Details
References

Tool Details

*FOR RESEARCH USE ONLY

  • Tool name: Glucose-6-phosphate Dehydrogenase inhibitor G6PD Small Molecule (Collaborative Toolkit)
  • Cancer: Head and neck cancer;Digestive/Gastrointestinal cancer
  • Cancers detailed: Larynx;Gastric
  • Tool sub type: Inhibitor
  • Primary target: Glucose-6-phosphate dehydrogenase (G6PD)
  • 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. 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
  • Purpose: Inhibitor
  • 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
  • Molecular weight: 1.0 ÂľM
  • Solubility: 30-100ÂľM in PBS

Handling

  • Purity: 360.5 kDa

Target Details

  • Primary target: Glucose-6-phosphate dehydrogenase (G6PD)
  • Ic50: 1.0 ÂľM

Application Details

  • Application notes: Cell permeability: Caco2 Permeability: 31.6 x 10-6 cm/s (efflux ratio 0.54)

References

  • Hamilton et al. 2012. J Med Chem. 55(9):4431-45. PMID: 22506561.
  • Hitchin et al. 2012. Tetrahedron Letters. 53:2868-72