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.
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.
References:
- [1]. Emerling, B. M., et al. "The PI5P4K family of lipid kinases as therapeutic targets in cancer." Nature Reviews Cancer, 21(7), 467-484. (2021).
- [2]. Palamiuc L, et al. Hippo and PI5P4K signaling intersect to control the transcriptional activation of YAP. Sci Signal. 2024 May 28;17(838):eado6266. [Content Brief]
- [3]. Arora GK, Pet al. Expanding role of PI5P4Ks in cancer: A promising druggable target. FEBS Lett. 2022 Jan;596(1):3-16. [Content Brief]
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PI5P4K Related Products (20)
Related Products (20)
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NCT-504
0 ImagesNCT-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.
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PIP4K-IN-a131
0 ImagesPIP4K-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.
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NIH-12848
0 ImagesNIH-12848 is a putative phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor with an IC50 of 1 μM.
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LRK-4189
0 ImagesCat. No.: HY-175751CAS No.: 3063346-83-5LRK-4189 is an first-in-class, orally active CRBN-dependent PIP4K2C PROTAC degrader. LRK-4189-mediated degradation of PIP4K2C leads to intrinsic cell death and upregulation of the STAT1 pathway and signaling in microsatellite stable colorectal cancer (MSS CRC) cells. LRK-4189 can be used for the research of microsatellite-stable colorectal cancer.
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CVM-05-002
0 ImagesCVM-05-002 is a selective pan-phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) inhibitor, with IC50 values of 0.27 μM and 1.69 μM against PI5P4Kα and PI5P4Kβ, respectively. CVM-05-002 binds non-covalently to the ATP-binding pocket of PI5P4Kα, forming hydrophobic interactions and hydrogen bonds with pocket residues. CVM-05-002 can be used in tumor-related research.
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(Rac)-LRK-4189
0 ImagesCat. No.: HY-175751ACAS No.: 3063345-48-9
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PI5P4Kγ-IN-1
0 ImagesPI5P4Kγ-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.
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TM-04-176-01
0 ImagesSynonyms: PI5P4Kα-IN-1
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PI5P4K-β-IN-1
0 ImagesCat. No.: HY-149423CAS No.: 332407-28-0PI5P4K-β-IN-1 (compound vs1) is a potent inhibitor of PI5P4K-β (IC50: 0.80 μM).
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066ATZ
0 ImagesCat. No.: HY-183627066ATZ 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.
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PI5P4Ks-IN-3
0 ImagesCat. No.: HY-153529CAS No.: 2471969-07-8PI5P4Ks-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.
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TMX-4102
0 ImagesCat. No.: HY-174296TMX-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.
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