PI4K Inhibitor

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.

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.

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.

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.

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.

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.

PI4Kβ/PKG-IN-2 (Compound 20) is an orally active dual inhibitor of Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). PI4Kβ/PKG-IN-2 has potent inhibitory effects on Plasmodium. PI4Kβ/PKG-IN-2 is promising for research of malaria.

AL-9 is a inhibitor of PI4KIIIα, with the IC₅₀ of 0.57 μM, that can inhibit HCV replication.

UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC₅₀ of 23 nM.

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.

Pi4kb Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pi4kb gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

PI4KA Human Pre-designed siRNA Set A contains three designed siRNAs for PI4KA gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

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.

Echiguanine B is a phosphatidylinositol-4-kinase (PI4K) inhibitor with an IC₅₀ of 0.11 μg/mL against human targets. Echiguanine B inhibits phosphatidylinositol-4-kinase activity in the cell membranes of epithelial cancer cells. Echiguanine B can be used in cancer-related research.

KAI-407 is an orally active inhibitor of Plasmodium PI4K kinase, which can broadly inhibit multiple stages of the parasite lifecycle. KAI-407 exhibits EC₅₀s of for the blood stage of malignant Plasmodium of 81 nM; for the liver schizonts of P. yoelii of 88 nM; and IC₅₀s for the liver schizonts and dormant bodies of P. cynomolgi of 0.64 μM and 0.69 μM respectively. KAI-407 can prevent Plasmodium berghei infection 100%. KAI-407 can be used for the study of vivax malaria.

PI4KIII beta inhibitor 5 is a PI4KIIIβ inhibitor with an IC₅₀ of 19 nM. PI4KIII beta inhibitor 5 can induce cancer cell apoptosis (Apoptosis), cell cycle arrest at the G2/M phase, and autophagy (Autophagy) by inhibiting the PI3K/AKT pathway. PI4KIII beta inhibitor 5 has also demonstrated significant antitumor activity in the H446 xenograft model of small cell lung cancer. PI4KIII beta inhibitor 5 can be used for research in the field of cancer therapy.

Pi4ka Rat Pre-designed siRNA Set A contains three designed siRNAs for Pi4ka gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

PI4KB Human Pre-designed siRNA Set A contains three designed siRNAs for PI4KB gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Pi4ka Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pi4ka gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

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.