| 产品描述: | SP-100030 是一种有效的 NF-κB 和激活蛋白-1 (AP-1) 双抑制剂 (IC50 分别为 50 和 50 nM)。SP-10003 抑制 Jurkat和其他T细胞系产生的 IL-2、IL-8 和 TNF-α 的产生。SP-100030 降低小鼠胶原性关节炎 (CIA)。 |
| 体外研究: |
SP-100030 blocks the production of IL-2 and IL-8 in Jurkat T-cells at the same concentrations as seen in the luciferase assay (IC50≈30 nM). ELISA and RT-PCR confirmed that IL-2, IL-8, and TNF-alpha production by activated Jurkat and other T cell lines were inhibited by SP100030. |
| 体内研究: |
SP100030 (10 mg/kg/day; i.p.; day 21 to day 34) significantly decreased arthritis severity. |
| 参考文献: |
1. Sullivan RW, et al. 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'- bis(trifluoromethyl)phenyl)-carboxamide: a potent inhibitor of NF-kappa B- and AP-1-mediated gene expression identified using solution-phase combinatorial chemistry. J Med Chem. 1998;4 [2]. Gerlag DM, et al. The effect of a T cell-specific NF-kappa B inhibitor on in vitro cytokine production and collagen-induced arthritis. J Immunol. 2000;165(3):1652-1658. |
| 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 |
2.285 ml |
11.425 ml |
22.849 ml |
| 5 mM |
0.457 ml |
2.285 ml |
4.57 ml |
| 10 mM |
0.228 ml |
1.142 ml |
2.285 ml |
| 50 mM |
0.046 ml |
0.228 ml |
0.457 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。 |