Pyridone 6
Cat. No.:YN340157
CAS No. :457081-03-7
产品名称: | Pyridone 6 |
CAS No.: | 457081-03-7 |
Chemical Name: | 2-(1,1-dimethylethyl)-9-fluoro-1,6-dihydro-7H-benz[h]imidazo[4,5-f]isoquinolin-7-one |
Synonyms: | 吡啶酮6 |
分子量: | 309.34 |
分子式: | C₁₈H₁₆FN₃O |
SMILES: | FC1=CC2=C(C(NC=C3)=O)C3=C(N=C(C(C)(C)C)N4)C4=C2C=C1 |
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: | Pyridone 6 是一种pan-JAK抑制剂,有效抑制 JAK 激酶家族,作用于JAK2,TYK2,JAK3和JAK1,IC50分别为 1 nM,1 nM,5 nM 和 15 nM。 |
IC50和靶点: | [{name:"JAK2:1 nM (IC50)"},{name: "Tyk2:1 nM (IC50)"},{name: "JAK3:5 nM (IC50)"},{name: "Murine JAK1:15 nM (IC50)"},{name: "CDK2:3.3 μM (IC50)"},{name: "cAMP-dependent kinase:7.1 μM (IC50)"},{name: "Csk:2.1 μM (IC50)"},{name: "Hck:7.7 μM (IC50)"},{name: "Fyn T:0.5 μM (IC50)"},{name: "p38:11 μM (IC50)"},{name: "MAPK:1.78 μM (IC50)"},{name: "Mek:0.16 μM (IC50)"},{name: "IκB Kinase 2:0.3 μM (IC50)"},{name: "KDR:1.4 μM (IC50)"},{name: "Flt-1:1.52 μM (IC50)"},{name: "Flt-4:0.69 μM (IC50)"},{name: "FGFR:1.48 μM (IC50)"},{name: "FGFR2:0.94 μM (IC50)"},{name: "Tek:24 μM (IC50)"},{name: "PDGFR:1.49 μM (IC50)"},{name: "PKC(α):1.2 μM (IC50)"}] |
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Leonard, W.J., and O'Shea, J.J.JAKS AND STATS: Biological implicationsAnnu. Rev. Immunol.16,293-322(1998)
Yamaoka, K., Saharinen, P., Pesu, M., et al.The Janus kinases (Jaks)Genome Biol.5(12),253(2004)
Thompson, J.E., Cubbon, R.M., Cummings, R.T., et al.Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitorBioorg. Med. Chem. Lett.12(8),1219-1223(2002)
Nakagawa, R., Yoshida, H., Asakawa, M., et al.Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17J. Immunol.187(9),4611-4620(2011)