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Phosphatidylinositol-4-phosphate 5-kinase inhibitor PIP5K Small Molecule (Collaborative Toolkit)

Invented by Dr Martin Swarbrick at Cancer Research Technology

Info

Antigen/Gene or Protein Targets Phosphatidylinositol-4-phosphate 5-kinase (PIP5K)
Relevance 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
Modulatory Function Inhibitor
On Target IC50 PIP5Kα IC50: 0.011 µM
PIP5Kβ IC50: 0.004 µM
PIP5Kγ IC50: 0.001 µM
Selectivity PI4KCA IC50: 20.9 µM
PI4KCB IC50: 5.99 µM
PI3Kα IC50: 34.6 µM
Solubility and Solvent 15 µM (Aqueous)
Molecular Weight (kDa) 430.5
Cell Permeability Caco2 permeability: 4.49 x 10-6 cm/s (efflux ratio 3.3)
Research Area Cell Structure and Motility, Developmental Biology
Relevant Indications PI3K, PLC, Wnt, Fc-receptor, BAF
Negative Control Available No

References: 1 entry

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


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References: 1 entry

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


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References: 1 entry

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


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