2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. PI5P4K

PI5P4K

PIP4K

PI5P4K/PIP4K (phosphatidylinositol 5-phosphate 4-kinase) is a crucial enzyme in phosphoinositide metabolism, with three isoforms: PI5P4Kα, PI5P4Kβ, and PI5P4Kγ, encoded by the genes PIP4K2A, PIP4K2B, and PIP4K2C, respectively. These kinases phosphorylate phosphatidylinositol 5-phosphate (PI5P) to produce phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2), which is vital for various signaling pathways. PI5P4Ks modulate the levels of PI(4,5)P2 at intracellular membranes, essential for processes like endocytosis. The balance between PI5P and PI(4,5)P2 is critical for cellular responses to stress.
PI5P4Ks are involved in key signaling pathways, particularly the Hippo pathway, which regulates cell growth. the Hippo pathway kinases phosphorylated and suppressed the activity of PI5P4Ks. These two important evolutionarily conserved signaling pathways are integrated to regulate metazoan development and human disease. In cancer biology, PI5P4Ks exhibit dual roles. For instance, in prostate cancer, higher expression levels of PI5P4Kα correlate with lower androgen receptor signaling, suggesting a potential tumor-suppressive role 3. Conversely, in other contexts, they may promote tumor growth by enhancing survival pathways under stress conditions. The intricate balance of their activity could provide therapeutic targets for cancer treatment by manipulating these signaling pathways.

PI5P4K Related Products (18):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-136311
    NCT-504
    		Inhibitor 99.46%
    NCT-504 is a selective allosteric inhibitor of PIP4Kγ, with an IC50 of 15.8 μM. NCT-504 is potential for the research of Huntington's disease.
    NCT-504
  • HY-139868
    BAY-091
    		Inhibitor 98.45%
    BAY-091, a chemical probe, is a potent and highly selective inhibitor of the kinase PIP4K2A.
    BAY-091
  • HY-136310
    PIP4K-IN-a131
    		Inhibitor 99.42%
    PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 μM and 0.6 μM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways.
    PIP4K-IN-a131
  • HY-139188
    CC260
    		Inhibitor 99.45%
    CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research.
    CC260
  • HY-101423
    NIH-12848
    		Inhibitor 99.96%
    NIH-12848 is a putative phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor with an IC50 of 1 μM.
    NIH-12848
  • HY-183627
    066ATZ
    		Inhibitor
    066ATZ is a PIP4K2A/2B inhibitor with human PIP4K2A Ki 100 nM and PIP4K2B Ki 800 nM. 066ATZ binds to ATP-binding sites of PIP4K2A and PIP4K2B to block lipid kinase activity. 066ATZ can be used for the research of non-small cell lung cancer.
    066ATZ
  • HY-186111
    BAY-297
    		Inhibitor
    BAY-297 is a PIP4K2A inhibitor. BAY-297 binds to PIP4K2A in intact cells and cell lysates. BAY-297 serves as a chemical probe for investigating the PIP4K2A signaling pathway and its roles in physiological conditions such as cancer.
    BAY-297
  • HY-153789
    PI5P4Kγ-IN-1
    		Inhibitor 98.82%
    PI5P4Kγ-IN-1 is an ATP-competitive, highly selective chemical probe for PI5P4Kγ, with a Kd of 19 nM and an IC50 of 67 nM. PI5P4Kγ-IN-1 effectively inhibits PI5P4Kγ function and activates the mTORC1 signaling pathway in cells. PI5P4Kγ-IN-1 can be used in studies related to diseases such as breast cancer.
    PI5P4Kγ-IN-1
  • HY-153531
    TM-04-176-01
    		Inhibitor 99.60%
    PI5P4Kα-IN-1 (Compound 13) is a PI5P4Kinhibitor (IC50: 2 and 9.4 μM for PI5P4Kα and PI5P4Kβ). PI5P4Kα-IN-1 can be used for research of cancer, metabolic and immunological disorders.
    TM-04-176-01
  • HY-149659
    ARUK2007145
    		Inhibitor 98.16%
    ARUK2007145 is potent, cell-active dual inhibitor of the PI5P4Kα and PI5P4Kγ isoforms (pIC50: 7.3 and 8.1, respectively).
    ARUK2007145
  • HY-153526
    PI5P4Ks-IN-2
    		Inhibitor 99.78%
    PI5P4Ks-IN-2 is a inhibitor of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ). PI5P4Ks-IN-2 targets to PI5P4K isoforms with pIC50 values of <4.3 (PI5P4Kα), <4.6 (PI5P4Kβ), 6.2 (PI5P4Kγ), 0.32 (PI5P4Kγ+), respectively.
    PI5P4Ks-IN-2
  • HY-152155
    ARUK2001607
    		Inhibitor 98.15%
    ARUK2001607 is a selective phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor with a Kd of 7.1 nM. ARUK2001607 shows high selectivity over other >150 kinases.
    ARUK2001607
  • HY-153532
    CVM-05-002
    		Inhibitor
    CVM-05-002 is a PI5P4K inhibitor, with IC50 values of 0.27 μM and 1.7 μM for PI5P4Kα and PI5P4Kβ, respectively.
    CVM-05-002
  • HY-145689
    PI5P4Ks-IN-1
    		Inhibitor
    PI5P4Ks-IN-1 (compound 7) is an active compound with no detectable inhibition of the PI5P4K α or β isoforms.
    PI5P4Ks-IN-1
  • HY-149423
    PI5P4K-β-IN-1
    		Inhibitor
    PI5P4K-β-IN-1 (compound vs1) is a potent inhibitor of PI5P4K-β (IC50: 0.80 μM).
    PI5P4K-β-IN-1
  • HY-153529
    PI5P4Ks-IN-3
    		Inhibitor
    PI5P4Ks-IN-3 (compound 30) is a covalent inhibitor of PI5P4K with IC50s of 1.34 μM (PI5P4Kα)，and 9.9 μM (PI5P4Kβ)，respectively. PI5P4Ks-IN-3 shows weak cellular activity.
    PI5P4Ks-IN-3
  • HY-174296
    TMX-4102
    TMX-4102 is a highly selective phosphatidylinositol 5-phosphate 4-kinase type II gamma (PIP4K2C) binder. TMX-4102 has binding activity to PIP4K2C (Kd = 0.45 nM) and has no significant effect on other lipid and non-lipid kinases.TMX-4102 specifically binds to PIP4K2C, regulating its scaffold function rather than its enzymatic activity. TMX-4102 can be used as a tool molecule to study the biological function and potential therapeutic value of PIP4K2C.
    TMX-4102
  • HY-149424
    PI5P4K-β-IN-2
    		Inhibitor
    PI5P4K-β-IN-2 (compound d5) is a PI5P4K-β inhibitor (IC50 = 0.35 μM) with antitumor activity.
    PI5P4K-β-IN-2