EN6 是一种小分子体内自噬激活剂，其共价靶向溶酶体v-ATP酶的 ATP6V1A 亚基中的半胱氨酸 277。它以溶酶体依赖性方式清除 TDP-43 聚集体，这是额颞叶痴呆的病原体。它介导的 ATP6V1A 修饰使 v-ATP 酶与 Rags 分离，从而抑制 mTORC1 信号传导、增加溶酶体酸化和激活自噬。

EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner. EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H+ ATPase (v-ATPase).

1808714-73-9

C19H14F2N4O2

368.34

DMSO:4.63 mg/mL (12.57 mM),Need ultrasonic
Ethanol:1.10 mg/mL (2.99 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years