| 产品描述: | BC-1215 是一种 F-box protein 3 (Fbxo3, a ubiquitin E3 ligase component) 的抑制剂,对于IL-1β释放的IC50值 为0.9 μg/mL,LC50值为87 μg/ml。BC-1215 通过破坏 TRAF1-6 的稳定性来抑制 Fbxo3-TRAF 激活途径 |
| 靶点: |
IL-1β release(Cell-free assay):0.9 μg/mL; IL-1β release(Cell-free assay):87 μg/mL(LC50);LigandforE3Ligase |
| 体外研究: |
BC-1215, a Fbxo3 inhibitor, inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6 proteins. Also, BC-1215 inhibits LPS-induced secretion of a broad spectrum of TH1 panel cytokines in human PBMC |
| 体内研究: |
A small molecule Fbxo3 inhibitor, BC-1215, reduces inflammation by antagonizing actions of Fbxo3 on TRAF–cytokine signaling |
| 细胞实验: |
Cell lines: Murine lung epithelial (MLE) cells, PBMC, U937 cells Concentrations: -- Incubation Time: -- Method: Murine lung epithelial (MLE) cells were treated with benzathine or BC-1215 at different concentrations for 16 h. Cells were collected and assayed for TRAF1-6, Fbxl2, Fbxo3, and actin immunoblotting. PBMC were treated with either vehicle or 2 μg/ml LPS for 18 h, some cells were also co-treated with BC-1215 in a dose dependent manner up to 10 μg/ml. 18 h later, cells were collected and processed for TRAF immunoblots. U937 cells were transfected with either empty or Fbxo3 plasmid for 24 h. Cells were also treated with BC-1215 in a dose dependent manner up to 10 μg/ml. 18 h later, cells were collected and processed for TRAF immunoblots. PBMC (0.6 ml at 1.5 x 106/ml) were treated with 2 ug/ml LPS for 16 h with BC-1215 at 10 μg/ml. Cytokine release was monitored by the human cytokine array. |
| 动物实验: |
Animal Models: model of a cecal ligation and puncture (CLP)-induced sepsis Dosages: 100 μg Administration: i.p. |
| 参考文献: |
1. Bill B Chen, et al. A combinatorial F box protein directed pathway controls TRAF adaptor stability to regulate inflammation. Nat Immunol. 2013 May;14(5):470-9. |
| 溶解性: |
Soluble in DMSO、Ethanol |
| 保存条件: |
2-8°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.535 ml |
12.674 ml |
25.348 ml |
| 5 mM |
0.507 ml |
2.535 ml |
5.07 ml |
| 10 mM |
0.253 ml |
1.267 ml |
2.535 ml |
| 50 mM |
0.051 ml |
0.253 ml |
0.507 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。 |