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Contributor Information

  • Institute Cancer Research Technology – AstraZeneca Metabolism Alliance Team

Tool Details

  • Tool name: Phosphatidylinositol-4-phosphate 5-kinase inhibitor PIP5K Small Molecule (Collaborative Toolkit)
  • Tool type: Small molecules
  • Tool sub-type: Inhibitor
  • Purpose: Inhibitor
  • Molecular weight of the target: PIP5KÎą IC50: 0.011 ÂľM PIP5Kβ IC50: 0.004 ÂľM PIP5KÎł IC50: 0.001 ÂľM
  • Description: A selective inhibitor of phosphatidylinositol-4-phosphate 5-kinase (PIP5K) which demonstrates anti-cancer activity. The PIP5K isoforms are PtdIns4P 5-kinases that endogenously synthesise the secondary messenger PtdIns(4,5)P2. PtdIns(4,5)P2 is involved in a wide variety of biological processes, including development, endocytosis, actin dynamics, chemotaxis, and Ins(1,4,5)P3 formation. The distinct subcellular localizations of these proteins indicate that specific PIP5K isoforms interact with particular components in a given subcellular compartment and produce function-specific pools of PtdIns(4,5)P2. The PIP5K subfamily is known to be involved in diverse cellular functions including embryonic development via the Wnt pathway, endocytosis, regulation of the actin cytoskeleton, and chemotaxis via impairment of cellular polarization. Synonyms for Phosphatidylinositol-4-phosphate 5-kinase: PIKFYVE, Phosphoinositide Kinase, FYVE Finger Containing Phosphatidylinositol-3-Phosphate/Phosphatidylinositol 5-Kinase Type III, Phosphatidylinositol 3-Phosphate 5-Kinase Type III, Type III PIP Kinase, PIPkin-III, PIP5K3, FYVE Finger-Containing Phosphoinositide Kinase 4, 1-Phosphatidylinositol-3-Phosphate 5-Kinase, Phosphatidylinositol 3-Phosphate 5-Kinase, Zinc Finger FYVE Domain Containing, Epididymis Luminal Protein 37, FYVE Domain Containing 29, KIAA0981, ZFYVE29, PIKfyve, HEL37, PIP5K, FAB1, CFD
  • Selectivity: PI4KCA IC50: 20.9 ÂľM PI4KCB IC50: 5.99 ÂľM PI3KÎą IC50: 34.6 ÂľM
  • IC50: PIP5KÎą IC50: 0.011 ÂľM PIP5Kβ IC50: 0.004 ÂľM PIP5KÎł IC50: 0.001 ÂľM

  • For Research Use Only

Target Details

  • Target molecular weight: PIP5KÎą IC50: 0.011 ÂľM PIP5Kβ IC50: 0.004 ÂľM PIP5KÎł IC50: 0.001 ÂľM
  • Primary target: Phosphatidylinositol-4-phosphate 5-kinase (PIP5K)

Application Details

  • Application notes: Cell Permeability: Caco2 permeability: 4.49 x 10-6 cm/s (efflux ratio 3.3)

Handling

  • Purity: 430.5 kDa
  • Solubility: 15 ÂľM (Aqueous)

Documentation

  • Available on request

References

  •   Andrews et al. 2014. Eur. J. Cancer. 50(6):91