2. Signaling Pathways
  3. PI3K/Akt/mTOR
  4. PI4K

PI4K

Phosphatidylinositol 4 kinases; PI4 kinases

PI4K

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Phosphatidylinositol 4-kinases (PI4Ks) catalyze the synthesis of phosphatidylinositol 4-phosphate (PI4P), an important intermediate for the synthesis of membrane polyphosphoinositides, regulators of multiple cellular functions. PI4P defines the membranes of Golgi and trans-Golgi network (TGN) and regulates trafficking to and from the Golgi. Based on enzymatic differences, two classes of PI4K have been distinguished termed Types II (PI4KII) and III (PI4KIII), and each of which contains α and β isoforms.

PI4KII alpha and beta have similar biochemical properties. PI4KIIIs (α- and β-forms) are soluble enzymes structurally related to PI3-kinases, and sensitive to PI3-kinase inhibitors, such as Wortmannin. PI4KIIs produce PtdIns 4-phosphate, an early key signaling molecule in phosphatidylinositol cycle, which is indispensable for T cell activation. PI4KIIIs plays a key role in the production of replication complexes (viral factories) of a number of positive-sense RNA viruses and represents a potential target for novel pan-viral therapeutics.

PI4K Isoform Specific Products:

PI4K Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-103489
    PI-273
    		Inhibitor 98.47%
    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.
    PI-273
  • HY-125118
    GSK-A1
    		Inhibitor 99.04%
    GSK-A1 is a selective type III phosphatidylinositol 4-kinase PI4KA (PI4KIIIα) inhibitor with a pIC50 of 8.5-9.8. GSK-A1 inhibits PtdIns(4,5)P2 resynthesis with an IC50 of about 3 nM. GSK-A1 potently decreases the levels of PtdIns(4)P with a negligible effect on PtdIns(4,5)P2. GSK-A1 has the potential for anti-hepatitis C virus (HCV) research.
    GSK-A1
  • HY-U00426
    BF738735
    		Inhibitor 99.26%
    BF738735 is a phosphatidylinositol 4-kinase III beta (PI4KIIIβ) inhibitor with an IC50 of 5.7 nM.
    BF738735
  • HY-12046
    PIK-93
    		Inhibitor 99.81%
    PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
    PIK-93
  • HY-100198
    PI4KIIIbeta-IN-10
    		Inhibitor 99.84%
    PI4KIIIbeta-IN-10 is a potent PI4KIIIβ inhibitor with an IC50 of 3.6 nM.
    PI4KIIIbeta-IN-10
  • HY-182721
    Pipinib
    		Inhibitor
    Pipinib 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.
    Pipinib
  • HY-N19295
    Echiguanine A
    		Inhibitor
    Echiguanine 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.
    Echiguanine A
  • HY-179469
    KR-27452
    		Inhibitor
    KR-27452 is a selective and orally active PI4KIIIβ inhibitor with an IC50 of 0.026 μM, while showing no activity against PI4KIIIα (IC50 >10 μM) . KR-27452 specifically binds to and inhibits PI4KIIIβ, leading to reduced viral replication in cells. KR-27452 exhibits strong antiviral activity against human rhinovirus (RVs) and Coxsackievirus (COXs). KR-27452 can be used for the research of infection.
    KR-27452
  • HY-106012
    PI4K-IN-1
    		Inhibitor 98.61%
    PI4K-IN-1 (compound 44) is a potent PI4KIII inhibitor, with pIC50 values of 9.0 and 6.6 for PI4KIIIα and PI4KIIIβ, respectively. PI4K-IN-1 also inhibits PI3Kα/β/γ/δ, with pIC50 values of 4.0/<3.7/5.0/<4.1, respectively.
    PI4K-IN-1
  • HY-115675
    NC03
    		Inhibitor 98.79%
    NC03 is a PI4K2A inhibitor and reducing agent. NC03 inhibits the activity of PI4K2A, thereby reducing the production of PI4P in the cellular compartments where PI4K2A functions. NC03 rapidly induces a decrease in PI4P pools in the Golgi and endosomal compartments. NC03 reduces PI4P production in Rab7-positive late endosomes.
    NC03
  • HY-19798
    PI4KIIIbeta-IN-9
    		Inhibitor 99.18%
    PI4KIIIbeta-IN-9 is a potent PI4KIIIβ inhibitor with an IC50 of 7 nM. PI4KIIIbeta-IN-9 also inhibits PI3Kδ and PI3Kγ with IC50s of 152 nM and 1046 nM, respectively.
    PI4KIIIbeta-IN-9
  • HY-108313
    T-00127_HEV1
    		Inhibitor 99.97%
    T-00127_HEV1 is a phosphatidylinositol 4-kinase III beta (PI4KB) inhibitor with an IC50 of 60 nM.
    T-00127_HEV1
  • HY-100603
    GSK-F1
    		Inhibitor
    GSK-F1 (Compound F1) is an orally active PI4KA inhibitor with pIC50 values of 8.0, 5.9, 5.8, 5.9, 5.9 and 6.4 against PI4KA, PI4KB, PI3KA, PI3KB, PI3KG and PI3KD, respectively. GSK-F1 can be used for HCV infection research.
    GSK-F1
  • HY-12912
    KDU691
    		Inhibitor 99.09%
    KDU691, an imidazopyrazine with potent anti-parasitic activity against blood stage schizonts, gametocytes and liver stages, is a Plasmodium PI4K inhibitor. KDU691 selectively inhibits dihydroartemisinin-pretreated Plasmodium falciparum ring-stage parasites.
    KDU691
  • HY-112613
    UCB9608
    		Inhibitor 99.59%
    UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent.
    UCB9608
  • HY-106005
    MMV390048
    		Inhibitor 98.85%
    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.
    MMV390048
  • HY-15679
    PI4KIII beta inhibitor 3
    		Inhibitor 99.36%
    PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC50 of 5.7 nM.
    PI4KIII beta inhibitor 3
  • HY-156685
    EDI048
    		Inhibitor 99.86%
    EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children.
    EDI048
  • HY-110248
    MI 14
    		Inhibitor 99.30%
    MI 14 is a selective PI4KIIIβ inhibitor with IC50s of 54 nM, >100 μM, >100 μM for PI4KIIIβ, PI4KIIIα, PI4KIIα, respectively. MI 14 has antiviral activity against HCV 1b, CVB3, HRVM, HVC 2a.
    MI 14
  • HY-150023
    BI-1622
    		Inhibitor
    BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.
    BI-1622
PI4K Isoform Comparison

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