FMK-9a

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

FMK-9a (FMK9a) 是一种有效的、选择性的、ATG4B (Autophagin-1) 共价拟肽抑制剂，TR-FRET 测定中的 IC50 为 80 nM；对天冬氨酸蛋白酶、丝氨酸蛋白酶、金属蛋白酶和 20S 蛋白酶体没有活性，抑制组织蛋白酶 B 和钙蛋白酶，IC50 为亚微摩尔 (0.1-0.2 uM)；与 Cys74 共价结合并灭活 ATG4B 蛋白水解活性，在细胞 LRA 测定中的 IC50 为 15 nM。

FMK-9a (FMK9a)?is a potent, selective, covalent peptidomimetic inhibitor of ATG4B (Autophagin-1) with IC50 of 80 nM in TR-FRET assay; displays no activity against the aspartic protease, serine proteases, metalloproteases and the 20S proteasome, inhibits cathepsin B and calpain with submicromolar IC50 (0.1-0.2 uM); covalently binds to Cys74 and inactivates ATG4B proteolytic activity, has an IC50 of 15 nM in the cellular 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.

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.

FMK 9a | FMK9a

Autophagy

Atg

Atg

——

——

1955550-51-2

392.4229

C23H21FN2O3

>98% (HPLC)

DMSO: ≥ 150 mg/mL

O=C(C1=C2C=CC=CC2=CC=C1)N[C@@H](CC3=CC=CC=C3)C(NCC(CF)=O)=O

1-Naphthalenecarboxamide, N-[(1S)-2-[(3-fluoro-2-oxopropyl)amino]-2-oxo-1-(phenylmethyl)ethyl]-

(-20℃)

With Ice Pack

≥ 2 years