Nur77 modulator 1 能够与 Nur77 结合(KD = 3.58 μM),上调其表达,调控 Nur77 的亚细胞定位,诱导 Nur77 依赖的内质网应激和自噬,从而引起细胞凋亡,并表现出抗肝癌的生物活性。
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描述 | 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) triggers Nur77-dependent apoptosis[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]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.02mL 0.40mL 0.20mL |
10.09mL 2.02mL 1.01mL |
20.18mL 4.04mL 2.02mL |
CAS号 | 2469975-55-9 |
分子式 | C28H25N5O2S |
分子量 | 495.6 |
SMILES Code | O=C(C(N1)=CC2=C1C=CC(NC3=CC(C)=NC4=C(OC)C=CC=C34)=C2)N/N=C/C5=CC=C(SC)C=C5 |
别名 | |
运输 | 蓝冰 |
InChI Key | ZDSQJUKYFCIYLG-MUFRIFMGSA-N |
Pubchem ID | 155971225 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
DMSO: 120 mg/mL(242.13 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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