DIM-C-pPhOH是核受体 NR4A1 的拮抗剂,抑制 mTOR 信号传导并诱导细胞凋亡,IC50 对 ACHN 和 786-O 细胞分别为 13.6 μM 和 13.0 μM。
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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]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.96mL 0.59mL 0.30mL |
14.78mL 2.96mL 1.48mL |
29.55mL 5.91mL 2.96mL |
CAS号 | 151358-47-3 |
分子式 | C23H18N2O |
分子量 | 338.402 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Sealed in dry,Room Temperature |
溶解方案 |
DMSO: 120 mg/mL(354.61 mM),配合低频超声,并水浴加热至45℃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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动物实验配方 |