产品说明书
DIM-C-pPhCO2Me
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同义名 : | - |
| CAS号 : | 151358-48-4 | |
| 货号 : | A1145756 | |
| 分子式 : | C25H20N2O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 380.44 | |
| MDL号 : | MFCD31697720 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 120 mg/mL(315.42 mM)，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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | NR4A1 is an orphan nuclear receptor which can activate mTOR signaling and exhibits pro-oncogenic activity in cancer cell lines, 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-pPhCO2Me is a NR4A1 antagonist. DIM-C-pPhCO2Me exhibited anti-proliferative effect on ACHN cells and 786-O cells with IC50 values of 11.7μM and 13.4μM, respectively, as well as induced apoptosis in both cell lines at concentration of 20μM post 24h. DIM-C-pPhCO2Me at concentration of 20μM inhibited NR4A1-regulated expression of survivin, bcl-2 and EGFR, decreased expression of TXNDC5 and IDH1, and induced stress shown by increased CHOP, ATF4 and p-PERK. Inhibition of NR4A1 by 20μM DIM-C-pPhCO2Me activated induced sestrin 2, activated AMPKα and inhibited activation of mTOR and downstream kinases including phosphorylation of p70S6K, S6RP and 4EBP1. Treatment with DIM-C-pPhCO2Me at concentration of 15μM or 20μM for 12h induced ROS production in Rh30 and RD cells. | ||
| 作用机制 | DIM-C-pPhCO2Me decreased interactions of NR4A1, p300 and pol II with the GC-rich TXNDC5 and IDH1 promoters and resulted in some loss of Sp1 from the TXNDC5 promoter.[2] | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.63mL 0.53mL 0.26mL |
13.14mL 2.63mL 1.31mL |
26.29mL 5.26mL 2.63mL |
| 参考文献 |
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