| Identification | Back Directory | [Name]
GSK-A1 | [CAS]
1416334-69-4 | [Synonyms]
GSK-A1
PI4KA inhibitor-A1
5-{2-Amino-1-[4-(4-morpholinyl)phenyl]-1H-benzimidazol-6-yl}-N-(2-fluorophenyl)-2-methoxy-3-pyridinesulfonamide
3-Pyridinesulfonamide, 5-[2-amino-1-[4-(4-morpholinyl)phenyl]-1H-benzimidazol-6-yl]-N-(2-fluorophenyl)-2-methoxy- | [Molecular Formula]
C29H27FN6O4S | [MDL Number]
MFCD29770784 | [MOL File]
1416334-69-4.mol | [Molecular Weight]
574.63 |
| Hazard Information | Back Directory | [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 has?the?potential?for?anti-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) |
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