| 产品描述: | AR antagonist 1 (compound 29) 是一种有效的 AR 拮抗剂,与 E3 连接酶配体结合,与 VHL 蛋白结合亲和力较弱,用于合成PROTAC ARD-266 (HY-133020)。 |
| 靶点: |
IC50: androgen receptor;AndrogenReceptor;LigandforE3Ligase;LigandsforTargetProteinforPROTAC |
| 体外研究: |
AR antagonist 1 (compound 29) is the ligand for target ligase of ARD-266. ARD-266 is a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. AR antagonist 1 exhibits micromolar binding affinity to its E3 ligase complex, it can be successfully employed for the design of highly potent and efficient PROTAC degraders. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins |
| 参考文献: |
1.Han X, et al. Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J Med Chem. 2019 Dec 26;62(24):11218-11231. |
| 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 |
3.587 ml |
17.935 ml |
35.871 ml |
| 5 mM |
0.717 ml |
3.587 ml |
7.174 ml |
| 10 mM |
0.359 ml |
1.794 ml |
3.587 ml |
| 50 mM |
0.072 ml |
0.359 ml |
0.717 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。 |