產(chǎn)品描述: | FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay. |
靶點: |
IC50: 80 nM (autophagin-1, FRET assay); 73 nM (autophagin-1, LRA assay);CysteineProtease;?Autophagy |
體外研究: |
ATG4B or autophagin-1 is a cysteine protease that cleaves ATG8 family proteins. ATG4B plays essential roles in the autophagosome formation and the autophagy pathway. FMK 9a shows strong inhibition of ATG4B, with IC50 values of 80 and 73 nM in the TR-FRET and cellular-based LRA assays, respectively. LC?MS/MS study indicates that FMK 9a forms an irreversible covalent bond with the more reactive thiol group of Cys74 located at the catalytic site of ATG4B and thus inactivates ATG4B proteolytic activity |
體內(nèi)研究: |
FMK 9a shows moderate solubility (LYSA: 41 μg/mL) and high human and mouse liver microsome clearances of 13.9 and 70 mL/kg per minute |
參考文獻: |
1. Qiu Z, et al. Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors. ACS Med Chem Lett. 2016 Jun 25;7(8):802-6. |
溶解性: |
soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.548 ml |
12.741 ml |
25.483 ml |
5 mM |
0.51 ml |
2.548 ml |
5.097 ml |
10 mM |
0.255 ml |
1.274 ml |
2.548 ml |
50 mM |
0.051 ml |
0.255 ml |
0.51 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |