| 产品描述： | Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases. |
| 靶点： |
JAK2:1 nM (IC50);Tyk2:1 nM (IC50);JAK3:5 nM (IC50);Murine JAK1:15 nM (IC50);CDK2:3.3 μM (IC50);cAMP-dependent kinase:7.1 μM (IC50);Csk:2.1 μM (IC50);Hck:7.7 μM (IC50);Fyn T:0.5 μM (IC50);p38:11 μM (IC50);MAPK:1.78 μM (IC50);Mek:0.16 μM (IC50);IκB Kinase 2:0.3 μM (IC50);KDR:1.4 μM (IC50);Flt-1:1.52 μM (IC50);Flt-4:0.69 μM (IC50);FGFR:1.48 μM (IC50);FGFR2:0.94 μM (IC50);Tek:24 μM (IC50);PDGFR:1.49 μM (IC50);PKC(α):1.2 μM (IC50) |
| 体内研究： |
Pyridone 6 (P6) delays the onset and reduced the magnitude of skin disease in an AD-like skin-disease model of NC/Nga mice. P6-nano strongly ameliorates atopic dermatitis (AD) in NC/Nga mice, exerting an effect comparable to that of betamethasone ointment, a commonly used drug, which also tested as a positive control. In contrast, empty polylactic acid with glycolic acid (PLGA) nanoparticles (C-nano) seemed to have no effect[ |
| 参考文献： |
1. Thompson JE, et al. Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorg Med Chem Lett. 2002 Apr 22;12(8):1219-23. 2. Nakagawa R, et al. Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17. J Immunol. 2011 Nov 1;187(9):4611-20. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.233 ml |
16.163 ml |
32.327 ml |
| 5 mM |
0.647 ml |
3.233 ml |
6.465 ml |
| 10 mM |
0.323 ml |
1.616 ml |
3.233 ml |
| 50 mM |
0.065 ml |
0.323 ml |
0.647 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京