Nur77 modulator 1 可与Nur77结合，KD为 3.58 μM。它上调 Nur77 表达，介导Nur77亚细胞定位，诱导Nur77 依赖的内质网应激和自噬，可导致细胞凋亡，Nur77 modulator 1显示出抗肝癌生物活性。

Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Nur77 modulator 1 shows anti-hepatoma activity.

Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines which are HepG2, QGY-7703, and SMMC-7721 respectively, and less cytotoxicity against LO2 cells (human normal liver cell line) [1]. Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner [1]. Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis [1] . Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete) [1] . Cell Viability Assay [1] . Cell Line: Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721). Concentration: 0-20 μM. Incubation Time: 12-24 hours. Result: Exhibited IC 50 values of 0.6 μM, 0.89 μM, 1.40 μM and >20 μM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively. Reduced the viability in a time-dependent manner. Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.

Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability [1]. Animal Model: Nude mouse hepatoma HepG2 xenograft [1]. Dosage: 10 and 20 mg/kg/day. Administration: IP, once every day for 15 days. Result: Lead to substantial suppression of tumor growth. The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. Exhibited almost no influence on the body weight of experimental mice. These results indicate that Nur77 modulator 1 has the potential to be developed as a novel Nur77-targeting anti-hepatoma drug.

2469975-55-9

C28H25N5O2S

495.6

Nur77 modulator 1;Nur77 modulator 1

DMSO:125 mg/mL (252.22 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years