GSK-A1

Product NameGSK-A1
CAS1416334-69-4
MFC29H27FN6O4S
MW574.63
EINECS
MOL File1416334-69-4.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMSO: 2 mg/ml
form	A solid
color	White to off-white
InChIKey	AJOGHKUZDLYXKS-UHFFFAOYSA-N
SMILES	O=S(C1=CC(C2=CC=C3C(N(C4=CC=C(N5CCOCC5)C=C4)C(N)=N3)=C2)=CN=C1OC)(NC6=CC=CC=C6F)=O

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

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 hasthepotentialforanti-hepatitis C virus (HCV) research[1].

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.

IC 50

PI4KA: 8.5-9.8 (pIC₅₀); PI4KB: 7.2-7.7 (pIC₅₀); PI4K2A: <5 (pIC₅₀); PI4K2B: <5 (pIC₅₀)

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)