| 产品描述： | NIK SMI1 is a potent, selective NF-κB inducing kinase (NIK) inhibitor, which inhibits NIK-catalyzed hydrolysis of ATP to ADP with IC50 of 0.23±0.17 nM |
| 靶点： |
NIK |
| 体外研究： |
NIK SMI1 (Compound 4f) inhibits NIK-catalyzed hydrolysis of ATP to ADP (fluorescence polarization, FP) with an IC50 of 0.23±0.17 nM. NIK SMI1 inhibits the expression of NIK SMI1 response elementregulated firefly luciferase reporter gene in HEK293 cells with an IC50 of 34±6 nM. Consistent with expectations for a NIK inhibitor, NIK SMI1 is shown to inhibit nuclear translocation of p52 (RelB) (IC50=70 nM). NIK SMI1 inhibits BAFF-induced B cell (mouse) survival in vitro with an IC50 of 373±64 nM. |
| 体内研究： |
C57BL/6 mice are treated twice daily for 7 days with orally administered NIK SMI1 or with three injections of recombinant BAFF receptor fusion protein (Br3- mIgG2a) over the course of the 7-day experiment as a positive control. The nonlinearity of exposure relative to dose between 100 and 200 mg/kg is a result of saturation of clearance mechanisms. The pharmacology of NIK SMI1 is examined in SD rat, CD-1 mouse, beagle, and cynomologous monkey with 20, 32, 18, and 7.8 mL/kg per min, respectively. Volume of distribution (Vd, L/kg) is 1.35, 1.58, 0.778, and 1.39, respectively. |
| 参考文献： |
1. Blaquiere N, et al. Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase. J Med Chem. 2018 Aug 9;61(15):6801-6813. |
| 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 |
2.737 ml |
13.684 ml |
27.369 ml |
| 5 mM |
0.547 ml |
2.737 ml |
5.474 ml |
| 10 mM |
0.274 ml |
1.368 ml |
2.737 ml |
| 50 mM |
0.055 ml |
0.274 ml |
0.547 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