GSK-A1

Biological Activity

GSK-A1 is an inhibitor of phosphatidylinositol 4-kinase IIIα (PI4KIIIα; IC50 = 3.16 nM).1 It is selective for PI4KIIIα over PI4KIIIβ, PI3Kα, PI3Kβ, and PI3Kδ (IC50s = >50 nM) but also inhibits PI3Kγ (IC50 = 15.8 nM). GSK-A1 decreases the levels of phosphatidylinositol 4-phosphate (PtdIns-(4)-P1) but not PtdIns-(4,5)-P2 in HEK293 cells expressing the angiotensin II type 1 (AT1) receptor (IC50 = 3 nM). GSK-A1 inhibits hepatitis C virus (HCV) genotype 1a and 1b replication.

References

1.Bojjireddy, N., Botyanszki, J., Hammond, G., et al.Pharmacological and genetic targeting of the PI4KA enzyme reveals its important role in maintaining plasma membrane phosphatidylinositol 4-phosphate and phosphatidylinositol 4,5-bisphosphate levelsJ. Biol. Chem.289(9)6120-6132(2014)