GSK2656157
Cat. No.：YN270269
CAS No. ：1337532-29-2
| 产品名称: | GSK2656157 |
| CAS No.: | 1337532-29-2 |
| Chemical Name: | 1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydro-1H-indol-1-yl]-2-(6-methyl-2-pyridinyl)-ethanone |
| Synonyms: | |
| 分子量: | 416.45 |
| 分子式: | C₂₃H₂₁FN₆O |
| SMILES: | CC1=CC=CC(CC(N2CCC3=C2C=CC(C4=CN(C)C5=NC=NC(N)=C54)=C3F)=O)=N1 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | GSK2656157 是选择性，ATP竞争性的PERK抑制剂，IC50值为 0.9 nM。 |
| IC50和靶点: | [{name:"EIF2AK3 (PERK):0.9 nM (IC50)"},{name: "EIF2AK1 (HRI):460 nM (IC50)"},{name: "BRK:905 nM (IC50)"},{name: "EIF2AK2 (PKR):905 nM (IC50)"},{name: "MEKK3:954 nM (IC50)"},{name: "Aurora B:1259 nM (IC50)"},{name: "KHS:1764 nM (IC50)"},{name: "LCK:2344 nM (IC50)"},{name: "MLK2:2796 nM (IC50)"},{name: "MEKK3:2847 nM (IC50)"},{name: "ALK5:3020 nM (IC50)"},{name: "MLCK2:3039 nM (IC50)"},{name: "EIF2AK4(GCN2):3162 nM (IC50)"},{name: "c-MER:3431 nM (IC50)"},{name: "PI3Kγ:3802 nM (IC50)"},{name: "WNK3:5951 nM (IC50)"},{name: "LRRK2:6918 nM (IC50)"},{name: "ROCK1:7244 nM (IC50)"},{name: "MSK1:8985 nM (IC50)"},{name: "NEK1:9807 nM (IC50)"},{name: "AXL:9808 nM (IC50)"},{name: "JAK2:24547 nM (IC50)"}] |
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Atkins, C., Liu, Q., Minthorn, E., et al.Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activityCancer Res.73(6),1993-2002(2013)
Axten, J.M., Romeril, S.P., Shu, A., et al.Discovery of GSK2656157: An optimized PERK inhibitor selected for preclinical developmentACS Med. Chem. Lett.4,964-968(2013)
Ando, T., Komatsu, T., Naiki, Y., et al.GSK2656157, a PERK inhibitor, reduced LPIS-induced IL-1b production through inhibiting caspase 1 activation in macrophage-like J774.1 cellsImmunopharmacol. Immunotoxicol.38(4),298-302(2016)
