PIK-93

Description

PIK-93 is an inhibitor of phosphatidylinositol 4-kinase IIIβ (PI4KIIIβ; IC₅₀ = 19 nM). It is selective for PI4KIIIβ over PI4KIIIα and PI4KIIα (IC₅₀s = 1,100 and >100,000 nM, respectively). However, it also inhibits the PI3K catalytic subunits (IC₅₀s = 39, 590, 120, and 16 nM for p110α, p110β, p110δ, and p110γ, respectively). PIK-93 reduces enteroviral RNA replication when used at a concentration of 125 nM in HeLa cells. It also inhibits the transport of ceramide from the endoplasmic reticulum to the Golgi apparatus.

The Uses of PIK-93

PIK 93 is a PI3Kγ and PI4KIIIβ inhibitor.

What are the applications of Application

PIK-93 is a novel and potent inhibitor

Enzyme inhibitor

This potent and selective PI3Kγ/PI4KIIIβ inhibitor (FW = 389.88; CAS 593960-11-3; Solubility (25°C): 78 mg/mL DMSO, <1 mg/mL Water), also known as N-[5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4- methylthiazol-2-yl]acetamide, impairs actin filament consolidation and stability at the leading edge in cells treated with N-formyl-Met-Leu-Phe as well as ceramide transport between ER and Golgi compartments. The inhibition of PI3K by PIK-93, LY294002, or wortmannin decreased carbachol-induced translocation of TRPC6 to the plasma membrane and carbachol-induced net Ca2+ entry into T6.11 cells. PIK-93 inhibits both poliovirus (PV) and hepatitis C virus (HCV) replication, with EC50 values of 0.14 μM and 1.9 μM, respectively. Targets: PI3Kγ, IC50 = 16 nM; PI4KIIIβ, IC50 = 19 nM; PI3Kα, IC50 = 39 nM; PI3Kδ, IC50 = 0.12 μM; and PI3Kβ, IC50 = 0.59 μM.

References

[1] monet m, francoeur n, boulay g. involvement of phosphoinositide 3-kinase and pten protein in mechanism of activation of trpc6 protein in vascular smooth muscle cells. j biol chem. 2012 may 18;287(21):17672-81.
[2] tóth b, balla a, ma h et al. phosphatidylinositol 4-kinase iiibeta regulates the transport of ceramide between the endoplasmic reticulum and golgi. j biol chem. 2006 nov 24;281(47):36369-77.
[3] hsu, n. y., et al. 2010. viral reorganization of the secretory pathway generates distinct organelles for rna replication. cell 141:799-811.
[4] arita m, kojima h, nagano t et al. phosphatidylinositol 4-kinase iii beta is a target of enviroxime-like compounds for antipoliovirus activity. j virol. 2011 mar;85(5):2364-72.