| 产品描述: | BRD7116 competitively binds to bacterial DNA gyrase, exhibits an EC50 of 200 nM for LSCe cells, with cell-non-autonomous anti-leukemia activity. IC50 value: 200 nM (EC50, for LSCe cells) Target: DNA gyrase BRD7116 is a bis-aryl sulfone, shows evidence of stroma-mediated anti-LSCe activity. BRD7116 exhibits an EC50 of 200 nM for LSCe cells in co-culture, whereas it displays limited activity against normal HSPCs and AML cell lines (~50% inhibition at 20 μM). BRD7116 also shows activity against patient-derived, primary human leukemia cells.BRD7116 inhibits LSCs via non-cell-autonomous effects on stromal cells as well as cell-autonomous induction of myeloid differentiation genes in LSCs. |
| 靶点: |
Bacterial;DNAgyrase;Antibacterial |
| 参考文献: |
1. Hartwell KA, et al. Niche-based screening identifies small-molecule inhibitors of leukemia stem cells. Nat Chem Biol. 2013 Dec;9(12):840-848 |
| 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 |
2.013 ml |
10.067 ml |
20.134 ml |
| 5 mM |
0.403 ml |
2.013 ml |
4.027 ml |
| 10 mM |
0.201 ml |
1.007 ml |
2.013 ml |
| 50 mM |
0.04 ml |
0.201 ml |
0.403 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。 |