PI5P4K
PIP4K
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.
- [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]
PI5P4K Isoform Specific Products
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PI5P4K Related Products (22)
Related Products (22)
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PI5P4K Isoform Comparison
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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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- BAY-091
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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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- CC260
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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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UNI418
0 ImagesUNI418 is a potent PIKfyve and PIP5K1C inhibitor with Kd values of 0.78 and 61 nM, respectively. UNI418 exhibits anti-SARS-CoV-2 activity with an EC50 of 1.4 μM. UNI418, through inhibition of PIKfyve and PIP5K1C (IC50 = 60.1 nM), on one hand lowers IP6 levels to trigger Cul4A-WDR5-dependent degradation of homologous recombination proteins, and on the other hand impedes endolysosomal acidification, cathepsin L maturation, and ACE2-mediated endocytosis, thereby blocking SARS-CoV-2 entry and escape. UNI418 can be used for research on ovarian cancer and SARS-CoV-2 infection. -
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TM-04-176-01
0 ImagesSynonyms: PI5P4Kα-IN-1 -
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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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ARUK2007145
0 ImagesCat. No.: HY-149659Purity: 98.16%ARUK2007145 is a PI5P4Kα and PI5P4Kγ inhibitor with pIC50 values of 7.3 and 8.1, respectively. ARUK2007145 is permeable, shows no efflux, has moderate solubility, and exhibits a high mouse liver microsomal metabolic rate. ARUK2007145 can be used in cancer-related research. -
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- PI5P4Ks-IN-2
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- ARUK2001607
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LRK-4189
0 ImagesCat. No.: HY-175751CAS No.: 3063346-83-5LRK-4189 is an 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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PIP4K ligand-1
0 ImagesCat. No.: HY-189438PIP4K ligand-1 is the target protein ligand for the molecular glue LRK-4189 (HY-175751) and can be used in research on microsatellite-stable colorectal cancer. -
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- TMX-4140
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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 PIP4K2C binder. TMX-4102 binds PIP4K2C with high affinity and high selectivity, with a Kd value of 0.45 nM, and can be used for research on lung adenocarcinoma. -
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