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| Product Name: | GSK-A1 | | Synonyms: | GSK-A1;PI4KA inhibitor-A1;3-Pyridinesulfonamide, 5-[2-amino-1-[4-(4-morpholinyl)phenyl]-1H-benzimidazol-6-yl]-N-(2-fluorophenyl)-2-methoxy-;5-{2-Amino-1-[4-(4-morpholinyl)phenyl]-1H-benzimidazol-6-yl}-N-(2-fluorophenyl)-2-methoxy-3-pyridinesulfonamide;PtdIns(4,5)P2,PI4KIIIα,inhibit,Hepatitis C virus,PI4K,GSK A1,GSK-A1,Phosphatidylinositol 4 kinases,PtdIns(4)P,phosphatidylinositol 4-kinase PI4KA,HCV,Inhibitor,PI4 kinases,GSKA1,GSK-A-1 | | CAS: | 1416334-69-4 | | MF: | C29H27FN6O4S | | MW: | 574.63 | | EINECS: | | | Product Categories: | | | Mol File: | 1416334-69-4.mol |  |
| | GSK-A1 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 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | GSK-A1 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) |
| | GSK-A1 Preparation Products And Raw materials |
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