PI4KIIIβ 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.

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.

BF738735 is a phosphatidylinositol 4-kinase III beta (PI4KIIIβ) inhibitor with an IC₅₀ of 5.7 nM.

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

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.

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.

T-00127_HEV1 is a phosphatidylinositol 4-kinase III beta (PI4KB) inhibitor with an IC₅₀ of 60 nM.

PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC₅₀ of 5.7 nM.

MI 14 is a selective PI4KIIIβ inhibitor with IC₅₀s of 54 nM, >100 μM, >100 μM for PI4KIIIβ, PI4KIIIα, PI4KIIα, respectively. MI 14 has antiviral activity against HCV 1b, CVB3, HRVM, HVC 2a.

BQR-695 is a PI4KIIIβ inhibitor with IC₅₀s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.

(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.

PI4KIIIbeta-IN-11 is an inhibitor of PI4KIIIβ, with a mean pIC₅₀ value of at least 9.1. PI4KIIIβ plays a key role in diseases research of RNA viruses and Plasmodium falciparum.

KR-27452 is a selective and orally active PI4KIIIβ inhibitor with an IC₅₀ of 0.026 μM, while showing no activity against PI4KIIIα (IC₅₀ >10 μM) . KR-27452 specifically binds to and inhibits PI4KIIIβ, leading to reduced viral replication in cells. KR-27452 exhibits strong antiviral activity against human rhinovirus (RVs) and Coxsackievirus (COXs). KR-27452 can be used for the research of infection.

PI4KIII beta inhibitor 4 (Compound 16) is a selective PI4KIIIβ inhibitor with an IC₅₀ of 0.005 μM. PI4KIIIβ inhibitor 4 induces tumor cell apoptosis, cell cycle arrest, and autophagy by inhibiting the PI3K/AKT pathway. PI4KIIIβ inhibitor 4 can be used in the study of cancer.

PI4K-IN-2 (Compound 30) is a highly selective type III phosphatidylinositol 4-kinase β (PI4KB) inhibitor (IC₅₀=0.015 μM). PI4K-IN-2 is promising for research of human rhinovirus (HRV).

PI4Kβ-IN-1 is an orally active and selective PI4Kβ inhibitor, with an IC₅₀ of 0.9 nM. PI4Kβ-IN-1 exhibits inhibitory activity against all stages of the P. falciparum life cycle, including blood, liver, and transmission stages. PI4Kβ-IN-1 demonstrates potent antimalarial efficacy in the mouse model infected with Plasmodium falciparum. PI4Kβ-IN-1 can be used for the study of malaria caused by Plasmodium falciparum.

KR-27370 (compound 7f) is an antiviral agent and selective PI4KIIIβ/PI4KIIIα inhibitor (IC₅₀: 3.1 nM/15.8 nM), against hRV, Ke Saatchivirus and other enteroviruses have inhibitory activity.