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。

FMK 9a is an autophagin-1 inhibitor with IC 50 values of 80 and 73 μM in FRET and LRA assay.

Solid

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

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 100 mg/mL (254.83 mM; Need ultrasonic)配制储备液