FMK-9A; FMK9A

中文名称:

FMK-9A; FMK9A

中文同义词:

AUTOPHAGIN-1抑制剂(FMK 9A)

英文名称:

FMK 9a

英文同义词:

FMK-9A; FMK9A;FMK 9a;1-Naphthalenecarboxamide, N-[(1S)-2-[(3-fluoro-2-oxopropyl)amino]-2-oxo-1-(phenylmethyl)ethyl]-

CAS号:

1955550-51-2

分子式:

C23H21FN2O3

分子量:

392.42

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1955550-51-2.mol

沸点 

724.6±60.0 °C(Predicted)

密度 

1.241±0.06 g/cm3(Predicted)

储存条件 

Inert atmosphere,2-8°C

酸度系数(pKa)

12.82±0.46(Predicted)

生物活性

FMK 9a是autophagin-1的抑制剂，在FRET和LRA试验中测定的IC50值分别为80 和73 nM。

靶点

IC50: 80 nM (autophagin-1, FRET assay); 73 nM (autophagin-1, LRA assay)

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 IC 50 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.