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PI3K/Akt/mTOR signalingPI4K
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.
UCT943
T132461450666-80-4
UCT943 is an inhibitor of Plasmodium falciparum PI4K (IC50 = 23 nM).
- $106
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GSK-F1
T198401402345-92-9
GSK-F1 (PI4KA inhibitor-F1) is a novel potent PI4KA inhibitor.
- $112
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T-00127_HEV1
T16967900874-91-1
T-00127_HEV1 is an inhibitor of phosphatidylinositol 4-kinase III beta (IC50: 60 nM).
- $51
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PI4KIIIbeta-IN-9
T124691429624-84-9
PI4KIIIbeta-IN-9 is a potent inhibitor of PI4KIIIβ [IC50 of 7 nM].
- $73
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PI-273
T12454925069-34-7
PI-273, a Substrate-Competitive, Specific Small-Molecule Inhibitor of PI4KIIα, Inhibits the Growth of Breast Cancer Cells
- $38
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AZ044
T266981800017-49-5
AZ044 is a potent, selective inhibitor of type III phosphatidylinositol-4-kinase alpha-subtype (PI4KIIIalpha).
- $52
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CHMFL-PI3KD-317
T108042244992-76-3
CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM, exhibiting over 10-1500 fold selectivity over other class I, II, and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM), and PI4KIIIB (IC50, 300.2 nM). It inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells with an EC50 of 4.3 nM and has antiproliferative effects on cancer cells.
- $93
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MMV390048
T161251314883-11-8
MMV390048 is an antimalarial agent and 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.
- $35
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BQR-695
T42201513879-21-4
BQR-695 (NVP-BQR695) is a phosphatidylinositol 4-kinase (PI4K) inhibitor with IC50s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.
- $64
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BF738735
T165301436383-95-7In house
BF738735 is a selective inhibitor of phosphatidylinositol 4-kinase III beta (PI4KIIIβ, IC50 = 5.7 nM) showing higher activity over α(IC50 = 1.7 μM). BF738735 exhibits a broad spectrum of antiviral activity.
- $40
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PIK-93
T2616593960-11-3
PIK-93, the first potent synthetic PI4K inhibitor, exhibits an IC50 of 19 nM and also inhibits PI3Kα with an IC50 of 39 nM.
- $37
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GSK-A1
T274991416334-69-4
GSK-A1 is a specific inhibitor of PI4KA, also inhibited calcium-driven PRL secretion without affecting calcium signaling and Prl expression. GSK-A1 has anti-hepatitis C virus (HCV) potential.
- $72
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(3S)-GSK-F1
T678371384097-27-1
(3S)-GSK-F1 is a selective small molecule inhibitor of Type III Phosphatidylinositol 4‑Kinase Alpha (PI4KIIIα), pIC50=8.3.
- $112
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UCB9608
TQ00091616413-96-7
UCB9608 is a selective and orally active PI4KIIIβ inhibitor (IC50: 11 nM), selective over PI3KC2 α, β, and γ lipid kinases.
- $50
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PI4KIIIbeta-IN-10
T124681881233-39-1
PI4KIIIbeta-IN-10 is a potent inhibitor of PI4KIIIβ with an IC50 value of 3.6 nM.
- $73
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LTURM34
T157891879887-96-3
LTURM34 is an inhibitor of DNA-PK with IC50 of 34 nM. LTURM34 displays effective antiproliferative activity in a wide range of tumor cell lines. LTURM34 shows 170-fold selectivity for DNA-PK over PI3K .
- $38
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EDI048
T798762767264-57-1
EDI048, also known as compound 1.16, is an orally active inhibitor of Cryptosporidium PI4K, utilized in the study of cryptosporidiosis [1].
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MIPS-21335
T817912569296-51-9
MIPS-21335 is a potent PI3KC2α inhibitor with an IC50 value of 7 nM and additionally exhibits inhibitory activity against PI3KC2β, p110α, p110β, and p110δ with IC50 values of 0.043, 0.140, 0.386, and 0.742 μM, respectively. This compound demonstrates an antithrombotic effect [1].
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