| 产品描述: | THS-044 binding stabilizes the HIF2α PAS-B folded state, for regulating HIF2 activity in endogenous and clinical settings. Target: HIF2α Limited trypsin proteolysis reveals that both apo and THS-044-bound protein are efficiently cut at R330 in the extended HI loop. In the THS-044 bound state, there appears no additional proteolysis at the remaining candidate trypsin sites. In contrast, these THS-044-protected sites are protease accessible in the unliganded protein, leading its complete degradation. In parallel, NMR-based deuterium exchange measurements revealed a dramatic stabilization of the THS-044-bound protein β-sheet, with some sites experiencing 100-fold enhanced protection factors relative to the ligand-free protein. |
| 靶点: |
HIF/HIF Prolyl-Hydroxylase |
| 参考文献: |
1: Motto I, Bordogna A, Soshilov AA, Denison MS, Bonati L. New aryl hydrocarbon receptor homology model targeted to improve docking reliability. J Chem Inf Model. 2011;51(11):2868-2881. doi:10.1021/ci2001617 2: Scheuermann TH, Tomchick DR, Machius M, Guo Y, Bruick RK, Gardner KH. Artificial ligand binding within the HIF2alpha PAS-B domain of the HIF2 transcription factor. Proc Natl Acad Sci U S A. 2009;106(2):450-455. doi:10.1073/pnas.0808092106 |
| 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 |
3.434 ml |
17.169 ml |
34.338 ml |
| 5 mM |
0.687 ml |
3.434 ml |
6.868 ml |
| 10 mM |
0.343 ml |
1.717 ml |
3.434 ml |
| 50 mM |
0.069 ml |
0.343 ml |
0.687 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。 |