Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,160 | 现货 | ||
5 mg | ¥ 2,860 | 现货 | ||
10 mg | ¥ 4,230 | 现货 | ||
25 mg | ¥ 6,780 | 现货 | ||
50 mg | ¥ 9,180 | 现货 | ||
100 mg | ¥ 12,300 | 现货 | ||
500 mg | ¥ 24,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,950 | 现货 |
产品描述 | 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. |
靶点活性 | Nur77:3.58 μM (KD) |
体外活性 | 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. |
体内活性 | 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. |
别名 | Nur77 modulator 1 |
分子量 | 495.6 |
分子式 | C28H25N5O2S |
CAS No. | 2469975-55-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (252.22 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0178 mL | 10.0888 mL | 20.1776 mL | 50.4439 mL |
5 mM | 0.4036 mL | 2.0178 mL | 4.0355 mL | 10.0888 mL | |
10 mM | 0.2018 mL | 1.0089 mL | 2.0178 mL | 5.0444 mL | |
20 mM | 0.1009 mL | 0.5044 mL | 1.0089 mL | 2.5222 mL | |
50 mM | 0.0404 mL | 0.2018 mL | 0.4036 mL | 1.0089 mL | |
100 mM | 0.0202 mL | 0.1009 mL | 0.2018 mL | 0.5044 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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