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PI4KA inhibitor-A1

Names

[ CAS No. ]:
1416334-69-4

[ Name ]:
PI4KA inhibitor-A1

[Synonym ]:
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-

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HCV
Research Areas >> Infection
Signaling Pathways >> PI3K/Akt/mTOR >> PI4K

[Target]

PI4KA:8.5-9.8 (pIC50)

PI4KB:7.2-7.7 (pIC50)

PI4K2A:<5 (pIC50)

PI4K2B:<5 (pIC50)


[References]

[1]. Naveen Bojjireddy, 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 levels. J Biol Chem. 2014 Feb 28;289(9):6120-32.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
829.8±75.0 °C at 760 mmHg

[ Molecular Formula ]:
C29H27FN6O4S

[ Molecular Weight ]:
574.626

[ Flash Point ]:
455.7±37.1 °C

[ Exact Mass ]:
574.179871

[ LogP ]:
4.18

[ Vapour Pressure ]:
0.0±3.0 mmHg at 25°C

[ Index of Refraction ]:
1.696

[ Storage condition ]:
-20°C

Related Compounds