|4-(二(1H-吲哚-3-基)甲基)苯酚|CsnPharm

CAS No.: 151358-47-3

4-(Di(1H-indol-3-yl)methyl)phenol Catalog No. CSN22788

Synonyms: C-DIM8;4-(Di(1H-indol-3-yl)methyl)phenol;1,1-bis-(3’-indolyl)-1-(p-hydroxyphenyl)methane

DIM-C-pPhOH is Nur77 antagonist which can induce conformational change.

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技术信息

生物活性

描述The orphan nuclear receptor NR4A1 (nuclear receptor 4A1) exhibits pro-oncogenic activity in cancer cell lines. NR4A1 activates mTOR signaling, regulates genes such as thioredoxin domain containing 5 and isocitrate dehydrogenase 1 that maintain low oxidative stress, and coactivates specificity protein 1 (Sp1)-regulated pro-survival and growth promoting genes. DIM-C-pPhOH binds NR4A1 and act as antagonists. DIM-C-pPhOH (20 μM; 18 hr) inhibited growth and induced apoptosis in ACHN and 786-O cells, and the functional and genomic effects of it were comparable to those observed after NR4A1 knockdown. Moreover, treatment of these cells with 0–20 μM of the NR4A1 antagonist DIM-C-pPhOH also significantly decreased cell proliferation. IC₅₀ values for DIM-C-pPhOH were 13.6 μM and 13.0 μM in ACHN cells and 786-O cells, respectively. Moreover, treatment of athymic nude mice bearing ACHN cells as xenografts with DIM-C-pPhOH (30 mg/kg/d) for 50 days also resulted in a significant inhibition of tumor growth and complemented results of the in vitro studies. In addition, researchers also observed decreased expression of survivin, bcl-2, EGFR and induced PARP cleavage in tumor lysates from nude mice bearing ACHN cells as a xenograft and treated with DIM-C-pPhOH (30 mg/kg/d)^[1].
参考文献

[1] Nuclear Receptor 4A1 (NR4A1) as a Drug Target for Renal Cell Adenocarcinoma

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9551 mL
- 14.7753 mL
- 29.5507 mL
- 5 mM
- 0.5910 mL
- 2.9551 mL
- 5.9101 mL
- 10 mM
- 0.2955 mL
- 1.4775 mL
- 2.9551 mL

技术信息

CAS号

151358-47-3

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H18N2O

运输

蓝冰

分子量

338.40

别名

C-DIM8;4-(Di(1H-indol-3-yl)methyl)phenol;1,1-bis-(3’-indolyl)-1-(p-hydroxyphenyl)methane

溶解度

DMSO	66.0 mg/mL (195.0 mM)
Water	Insoluble
Ethanol	66.0 mg/mL (195.0 mM)

动物实验配方

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