- Name Martin Swarbrick
- Institute Cancer Research Technology AstraZeneca Metabolism Alliance Team
- Tool name: Phosphatidylinositol-4-phosphate 5-kinase inhibitor PIP5K Small Molecule (Tool Compound)
- Alternate names: 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, KIAA981, ZFYVE29, PIKfyve, HEL37, PIP5K, FAB1, CFD
- Tool type: Small molecules
- Tool sub-type: Inhibitor
- Purpose: Inhibitor
- 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.
- Research area: Cancer
- Selectivity: PI4KCA IC50: 20.9 ÂľM PI4KCB IC50: 5.99 ÂľM PI3KÎą IC50: 34.6 ÂľM
- IC50: PIP5KÎą IC50: 0.011 ÂľM PIP5KÎ˛ IC50: 0.004 ÂľM PIP5KÎł IC50: 0.001 ÂľM
- Additional notes: Relevant Indications: PI3K, PLC, Wnt, Fc-receptor, BAF Negative Control Available: No The compounds are made up to 12mM stock concentration in DMSO. The final concentration of DMSO when treating cells should be less than 1%.
- For Research Use Only
- • Andrews et al. 2014. Eur. J. Cancer. 50(6):91