PI4K
PI4K enzymes catalyze conversion of phosphatidylinositol to phosphatidylinositol 4-phosphate (PI4P), and mammalian PI4KA, PI4KB, PI4K2A, and PI4K2B support intracellular lipid and protein trafficking[1]. Mechanistically, PI4P marks organelle identity and membrane trafficking pathways, while PI4KA and PI4KB regulate signaling, Golgi function, and viral replication through PI4P-enriched membrane systems[2]. In disease models, PI4KA supports hepatitis C virus membranous-web formation, whereas PI4KB supports positive-sense RNA virus replication and severe acute respiratory syndrome coronavirus spike-mediated entry[3][4][5]. Compared with related isoforms, PI4KA maintains plasma-membrane PI4P and phosphatidylinositol 4,5-bisphosphate under receptor stimulation, while PI4KB maintains Golgi and trans-Golgi network PI4P pools through ACBD3-dependent membrane recruitment[6][7]. For experimental applications, PI4K assays enable high-throughput inhibitor screening, and UCB9608 provides a potent, selective, orally bioavailable PI4KIIIβ inhibitor for probing PI4KB biology in vivo[1][8].
References:
- [1]. Tai AW, et al. A homogeneous and nonisotopic assay for phosphatidylinositol 4-kinases. Anal Biochem. 2011 Oct 1;417(1):97-102. [Content Brief]
- [2]. McPhail JA, et al. Molecular mechanisms of PI4K regulation and their involvement in viral replication. Traffic. 2023 Mar;24(3):131-145. [Content Brief]
- [3]. Tai AW, et al. The role of the phosphatidylinositol 4-kinase PI4KA in hepatitis C virus-induced host membrane rearrangement. PLoS One. 2011;6(10):e26300. [Content Brief]
- [4]. Dorobantu CM, et al. Mutations in Encephalomyocarditis Virus 3A Protein Uncouple the Dependency of Genome Replication on Host Factors Phosphatidylinositol 4-Kinase IIIα and Oxysterol-Binding Protein. mSphere. 2016 May 11;1(3):e00068-16. [Content Brief]
- [5]. Yang N, et al. Phosphatidylinositol 4-kinase IIIβ is required for severe acute respiratory syndrome coronavirus spike-mediated cell entry. J Biol Chem. 2012 Mar 9;287(11):8457-67. [Content Brief]
- [6]. Bojjireddy N, et al. Pharmacological and genetic targeting of the PI4KA enzyme reveals its important role in maintaining plasma membrane phosphatidylinositol 4-phosphate and phosphatidylinositol 4,5-bisphosphate levels. J Biol Chem. 2014 Feb 28;289(9):6120-32. [Content Brief]
- [7]. Klima M, et al. Structural insights and in vitro reconstitution of membrane targeting and activation of human PI4KB by the ACBD3 protein. Sci Rep. 2016 Mar 24;6:23641. [Content Brief]
- [8]. Reuberson J, et al. Discovery of a Potent, Orally Bioavailable PI4KIIIβ Inhibitor (UCB9608) Able To Significantly Prolong Allogeneic Organ Engraftment in Vivo. J Med Chem. 2018 Aug 9;61(15):6705-6723. [Content Brief]
All Product Categories
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PI4K Related Products (31)
Related Products (31)
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Pipinib
0 ImagesCat. No.: HY-182721CAS No.: 2380013-55-6Pipinib is an ATP-competitive and selective phosphatidylinositol 4-kinase IIIb (PI4KB) inhibitor with an IC50 of 2.2 μM. Pipinib reduces intracellular PI4P levels. Pipinib inhibits GLI-mediated transcription, the expression of Hedgehog target genes, and blocks the trafficking of Smoothened to cilia. Pipinib can be used in the research of basal cell carcinoma and medulloblastoma.
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Echiguanine A
0 ImagesCat. No.: HY-N19295CAS No.: 137319-25-6Echiguanine A is a phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.04 μg/mL. Echiguanine A inhibits phosphatidylinositol 4-kinase activity in cell membrane extracts. Echiguanine A is applicable for cancer research.
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PI4K-IN-3
0 ImagesCat. No.: HY-178775PI4K-IN-3 (Compound 27) is an orally active PI4K inhibitor with an IC50 of 1.9 nM for Plasmodium vivax PI4K. PI4K-IN-3 has no hERG channel inhibition and mammalian cytotoxicity. PI4K-IN-3 has significant selectivity against the human MINK1 and MAP4K4 kinases but with low selectivity against human PI3Kα and PI4Kβ. PI4K-IN-3 has potent antimalarial activity and significantly reduces parasitaemia in NSG mice mouse models of Plasmodium falciparum malaria.
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PI4KA-IN-1
0 ImagesCat. No.: HY-148956CAS No.: 1579232-30-6PI4KA-IN-1 (Compound G1) is a PI4KA inhibitor. PI4KA-IN-1 can be used in the research of hepatitis C virus infection.
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KDU731 (Standard)
0 ImagesCat. No.: HY-103583RCAS No.: 1610610-48-4KDU731 (Standard) is the analytical standard of KDU731 (HY-103583). This product is intended for research and analytical applications. KDU731, an orally active C. parvum PI4K inhibitor with an IC50 value of 25 nM, blocks Cryptosporidium infection in vitro and in vivo. KDU731 is a promising agent candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety.
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T-00127_HEV1 (Standard)
0 ImagesCat. No.: HY-108313RCAS No.: 900874-91-1T-00127_HEV1 (Standard) is the analytical standard of T-00127_HEV1 (HY-108313). This product is intended for research and analytical applications. T-00127_HEV1 is a phosphatidylinositol 4-Kinase III beta (PI4KB) inhibitor with an IC50 of 60 nM.
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PI4Kβ/PKG-IN-1
0 ImagesCat. No.: HY-174130PI4Kβ/PKG-IN-1 (Compound 19) is an orally active dual inhibitor targeting Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). PI4Kβ/PKG-IN-1 exhibits potent antiplasmodial activity. PI4Kβ/PKG-IN-1 is promising for research of malaria.
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MMV390048 (Standard)
0 ImagesCat. No.: HY-106005RCAS No.: 1314883-11-8MMV390048 (Standard) is the analytical standard of MMV390048 (HY-106005). This product is intended for research and analytical applications. MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 μM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent.
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PI-273 (Standard)
0 ImagesCat. No.: HY-103489RCAS No.: 925069-34-7PI-273 (Standard) is the analytical standard of PI-273 (HY-103489). This product is intended for research and analytical applications. PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis.
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(R)-GSK-F1
0 ImagesCat. No.: HY-100603BCAS No.: 1384097-28-2
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