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 ≥98.0%
    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-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-125118
    GSK-A1
    		Inhibitor ≥99.0%
    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 99.10%
    BF738735 is a phosphatidylinositol 4-kinase III beta (PI4KIIIβ) inhibitor with an IC50 of 5.7 nM.
    BF738735
  • HY-163765
    Antimalarial agent 41
    		Inhibitor
    Antimalarial agent 41 (Compound 17) exhibits antimalarial activity, which inhibits Plasmodium falciparum with an IC50 of 40 nM (NF54 strain) and 76 nM (K1 strain). Antimalarial agent 41 is an inhibitor for P. falciparum phosphatidylinositol-4-kinase β (Pf PI4K) and hERG channel, with an IC50 of 53 nM and 3 μM. Antimalarial agent 41 exhibits cytotoxicity to CHO cells with an IC50 of 34 μM. Antimalarial agent 41 ameliorates the malaria infection and exhibits good pharmacokinetic characters in mouse models.
    Antimalarial agent 41
  • HY-100603A
    (S)-GSK-F1
    		Inhibitor
    (S)-GSK-F1 (Compound 28) is an inhibitor for type III phosphatidylinositol 4-kinase α (PI4KIIIα). (S)-GSK-F1 inhibits PI4Kα, PI4Kβ, PI4Kγ, PI3Kα, PI3Kβ and PI3Kδ with pIC50 of 8.3, 6.0, 5.6, 5.6, 5.1 and 5.6, respectively. (S)-GSK-F1 exhibits anti-hepatitis C virus (HCV) activity through inhibition of HCV replication. (S)-GSK-F1 exhibits moderate pharmacokinetic characters in rat model.
    (S)-GSK-F1
  • 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-19798
    PI4KIIIbeta-IN-9
    		Inhibitor 99.01%
    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-106005
    MMV390048
    		Inhibitor 99.17%
    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 99.77%
    PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC50 of 5.7 nM.
    PI4KIII beta inhibitor 3
  • HY-12912
    KDU691
    		Inhibitor 99.42%
    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-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-18748
    BQR-695
    		Inhibitor 99.92%
    BQR-695 is a PI4KIIIβ inhibitor with IC50s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.
    BQR-695
  • HY-150023
    BI-1622
    		Inhibitor 98.97%
    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
  • 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-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-103583
    KDU731
    		Inhibitor 99.52%
    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.
    KDU731
  • HY-112435
    UCT943
    		Inhibitor 99.08%
    UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC50 of 23 nM.
    UCT943
  • HY-150598
    CHMFL-PI4K-127
    		Inhibitor 99.94%
    CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy.
    CHMFL-PI4K-127
PI4K Isoform Comparison

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