| 货号 | 15146-10mg |
| 描述 | Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors.1,2 JAK1 mostly activates IL-6, whereas JAK1 and JAK3 trigger IL-2 and IL-4 and JAK1 and JAK2 stimulates IFN-γ. JAK Inhibitor I is a pyridine-containing tetracycle that interferes with JAK kinase activity by interacting within the ATP-binding cleft. It inhibits JAK1, 2, and 3 with IC50 values of 15, 1, and 5 nM, respectively, while displaying significantly weaker affinities (IC50s = 130 nM - > 10 μM) for other protein tyrosine kinases.3 It was shown to block IL-2 and IL-4-dependent proliferation of mouse T-cell lymphoma cells with IC50 values of 50-100 nM.3 In a mouse model of atopic dermatitis, JAK Inhibitor I, supplied at 2 mg encapsulated in a PLGA nanoparticle, was shown to suppress IFN-γ/STAT1, IL-2/STAT5, and IL-4/STAT6 signaling pathways.4 |
| 别名 | CMP 6;Janus-Associated Kinase Inhibitor I;Pyridone 6; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Leonard, W.J. and OShea, J.J. JAKS AND STATS: Biological implications. Annual Reviews of Immunology 16, 293-322 (1998). 2.Yamaoka, K.,Saharinen, P.,Pesu, M., et al. The janus kinases (Jaks). Genome Biology 5(12), 1-6 (2004). 3.Thompson, J.E.,Cubbon, R.M.,Cummings, R.T., et al. Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorganic & Medicinal Chemistry Letters 12(8), 1219-1223 (2002). 4.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 Th17. Journal of Immunology 187(9), 4611-4620 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 309.3 |
| 分子式 | C18H16FN3O |
| CAS号 | 457081-03-7 |
| 稳定性 | ≥ 2 years |
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