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• 产品描述： FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.

• 靶点： IC50: 80 nM (autophagin-1, FRET assay); 73 nM (autophagin-1, LRA assay);CysteineProtease; Autophagy

• 体外研究：
  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

• 体内研究：
  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

• 参考文献：
  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

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *