PI5P4K Inhibitor

NCT-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.

BAY-091, a chemical probe, is a potent and highly selective inhibitor of the kinase PIP4K2A.

PIP4K-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.

CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with K_is of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research.

NIH-12848 is a putative phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor with an IC₅₀ of 1 μM.

UNI418 is an orally active and potent PIKfyve and PIP5K1C inhibitor with K_d 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 reduces IP6 levels to trigger Cul4A-WDR5-dependent homologous recombination protein degradation, and on the other hand impairs 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.

TM-04-176-01 (PI5P4Kα-IN-1) is a selective PIP4K2C inhibitor (K_d 3.4 nM) and PI5P4K inhibitor (IC50: 1.96 and 9.4 μM for PI5P4Kα and PI5P4Kβ, respectively). TM-04-176-01 inhibits SARS-CoV-2 replication with low cytotoxicity. TM-04-176-01 can be used for research on SARS-CoV-2 infection.

PI5P4Kγ-IN-1 is an ATP-competitive, highly selective chemical probe for PI5P4Kγ, with a K_d 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.

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.

PI5P4Ks-IN-2 is a inhibitor of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ). PI5P4Ks-IN-2 targets to PI5P4K isoforms with pIC₅₀ values of <4.3 (PI5P4Kα), <4.6 (PI5P4Kβ), 6.2 (PI5P4Kγ), 0.32 (PI5P4Kγ+), respectively.

ARUK2001607 is a selective phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor with a K_d of 7.1 nM. ARUK2001607 shows high selectivity over other >150 kinases.

CVM-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.

PI5P4K-β-IN-1 (compound vs1) is a potent inhibitor of PI5P4K-β (IC₅₀: 0.80 μM).

066ATZ is a PIP4K2A/2B inhibitor with human PIP4K2A K_i 100 nM and PIP4K2B K_i 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.

PI5P4Ks-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.

BAY-297 is a PIP4K2A inhibitor. BAY-297 binds to PIP4K2A in intact cells and cell lysates. BAY-297 serves as a chemical probe for investigating the PIP4K2A signaling pathway and its roles in physiological conditions such as cancer.

PI5P4K-β-IN-2 (compound d5) is a PI5P4K-β inhibitor (IC₅₀ = 0.35 μM) with antitumor activity.