Nur77 modulator 1 exhibits strong binding affinity for Nur77 (KD = 3.58 μM). It enhances Nur77 expression, regulates its sub-cellular localization, triggers Nur77-dependent ER stress and autophagy, ultimately leading to cell apoptosis. It demonstrates anti-hepatoma activity[1].
体内研究
Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) demonstrates notable anti-tumor efficacy in mouse hepatoma HepG2 xenograft models, with favorable tolerability[1].
体外研究
Nur77 modulator 1 (10g, 0-20 μM) exhibits strong and wide-ranging antiproliferative effects against all three tested hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), while showing lower cytotoxicity towards LO2 cells (human normal liver cell line)[1].
Nur77 modulator 1 (10g) can selectively increase the expression of Nur77 in a dose-dependent manner[1].
Nur77 modulator 1 (10g, 2.0 μM) dose-dependently elevated levels of LC3-II and Beclin1 proteins. However, 10g treatment did not enhance p62 degradation, suggesting incomplete induction of autophagy[1].
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