pi4kδ

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 .

PI4Kβ-IN-1 is an orally active selective inhibitor of PI4Kβ with an IC50 of 0.9 nM. It exhibits inhibitory activity across all stages of the P. falciparum lifecycle, including the blood, liver, and transmission phases. In mouse models infected with Plasmodium falciparum, PI4Kβ-IN-1 demonstrates significant antimalarial efficacy. This compound is applicable for research on malaria caused by Plasmodium falciparum.

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.

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.

PI-273, a Substrate-Competitive, Specific Small-Molecule Inhibitor of PI4KIIα, Inhibits the Growth of Breast Cancer Cells

PI4KIII beta inhibitor 3 is a novel, highly effective inhibitor of PI4KIIIβ with an IC50 of 5.7 nM.

PI4KIIIbeta-IN-10 is a potent inhibitor of PI4KIIIβ with an IC50 value of 3.6 nM.

PI4KIIIbeta-IN-9 is a potent inhibitor of PI4KIIIβ [IC50 of 7 nM].

UCT943 is an inhibitor of Plasmodium falciparum PI4K (IC50 = 23 nM).

KDU731 is a promising drug candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety. KDU731is an orally active C. parvum inhibitor of PI4K (IC50: 25 nM). KDU731 blocks Cryptosporidium infection in vitro and in vi

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.

T-00127_HEV1 is an inhibitor of phosphatidylinositol 4-kinase III beta (IC50: 60 nM).

GSK-F1 (PI4KA inhibitor-F1) is a novel potent PI4KA inhibitor.

PI4KIII beta inhibitor 4 (Compound 16) is a selective inhibitor of PI4KIIIβ with an IC50 of 0.005 μM. By inhibiting the PI3K/AKT pathway, PI4KIII beta inhibitor 4 induces apoptosis, causes cell cycle arrest, and triggers autophagy in tumor cells. This compound is applicable for tumor research.

PI4KIII beta inhibitor 5 (Compound 43) is an inhibitor of PI4KIIIβ with an IC50 of 19 nM. By inhibiting the PI3K/AKT pathway, it induces apoptosis in cancer cells, causes cell cycle arrest at the G2/M phase, and promotes autophagy. Additionally, PI4KIII beta inhibitor 5 demonstrates significant anti-tumor activity in the H446 small cell lung cancer xenograft model. This compound is applicable in cancer research studies.

PI4K-IN-3 (Compound 27) is an orally effective PI4K inhibitor with an IC50 of 1.9 nM for Plasmodium vivax PI4K. It does not inhibit the hERG channel and is non-cytotoxic to mammalian cells. This compound shows notable selectivity for human MINK1 and MAP4K4 kinases but has lower selectivity for human PI3Kα and PI4Kβ. PI4K-IN-3 exhibits potent antimalarial activity, significantly reducing parasitemia in NSG mouse models infected with Plasmodium falciparum.

PI4KA-IN-1 (Compound G1) is an inhibitor of PI4KA and is applicable in research related to hepatitis C virus (hepatitis C virus) infection.

AL-9 is a GT-1b and GT-2a replication inhibitor.

PIK-93, the first potent synthetic PI4K inhibitor, exhibits an IC50 of 19 nM and also inhibits PI3Kα with an IC50 of 39 nM.

AZ044 is a potent, selective inhibitor of type III phosphatidylinositol-4-kinase alpha-subtype (PI4KIIIalpha).

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.

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.

KDU691 is a PI4K inhibitor.

CHMFL-PI4K-127 (compound 15g) is a highly selective inhibitor of PfPI4K (Plasmodium falciparum PI4K kinase) with oral activity (IC50=0.9 nM) and exhibits strong inhibitory activity against Plasmodium falciparum 3D7 (EC50=25.1 nM), demonstrating significant anti-malaria effects.