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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDIM-C-pPhOHCat. No.: HY-112055CAS No.: 151358-47-3分式: CHNO分量: 338.4作靶点: Apoptosis作通路: Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthBIOLOGICAL ACTIVITY物活性 DIM-C-pPhOH核受体 4A1 (NR4A1) 拮抗剂。DIM-C-pPh

2、OH 抑制癌细胞的长和 mTOR 信号传导，诱导细胞凋亡和细胞应激。DIM-C-pPhOH 可降低细胞增殖，对 ACHN 细胞和 786-O 细胞的 IC50 值分别为 13.6 M和 13.0 M。IC50 & Target Nuclear receptor 4A1 (NR4A1) 1体外研究DIM-C-pPhOH (7.5-20 M; 24 hours; ACHN and 786-O cells) treatment significantly decreases cellproliferation 1.DIM-C-pPhOH (20 M; 24 hours; ACHN and 786-O

3、 cells) treatment induces Annexin V staining in ACHN and786-O cells, confirming that DIM-C-pPhOH induce apoptosis, and also induces cleavage of caspases 7 and 81.DIM-C-pPhOH (15-20 M; 24 hours; ACHN and 786-O cells) treatment inhibits NR4A1-regulated expressionof survivin, bcl-2 and EGFR in ACHN and

4、 786-O cells. And also induces sestrin 2, activates AMPK andinhibits activation of mTOR and downstream kinases 1.DIM-C-pPhOH decreases expression of 1-integrin protein and mRNA and 1-integrin-dependent responsesin MCF7, MDA-MB-231, and SKBR3 cells and also inhibits migration of the latter two cell l

5、ines 2.Cell Proliferation Assay 1Cell Line: ACHN and 786-O cells1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEConcentration: 7.5 M, 15 M, 20 MIncubation Time: 24 hoursResult: Significantly decreased cell proliferation.Apoptosis Analysis 1Cell Line: ACHN and 786-O cellsConcentration: 20 MIncubatio

6、n Time: 24 hoursResult: Induced apoptosis in ACHN and 786-O cells.Western Blot Analysis 1Cell Line: ACHN and 786-O cellsConcentration: 15 M, 20 MIncubation Time: 24 hoursResult: Inhibited NR4A1-regulated expression of survivin, bcl-2 and EGFR in ACHN and 786-Ocells. And also induced sestrin 2, activ

7、ated AMPK and inhibited activation of mTOR anddownstream kinases.体内研究 DIM-C-pPhOH (30 mg/kg; oral gavage; daily; for 50 days; male athymic nude mice) treatment results in asignificant inhibition of tumor growth 1.Animal Model: Male athymic nude mice (aged 6-7 weeks) injected with ACHN cells 1Dosage:

8、 30 mg/kg/dayAdministration: Oral gavage; daily; for 50 daysResult: Resulted in a significant inhibition of tumor growth.REFERENCES1. Hedrick E, et al. Nuclear Receptor 4A1 (NR4A1) as a Drug Target for Renal Cell Adenocarcinoma. PLoS One. 2015 Jun2;10(6):e0128308.2. Hedrick E, et al. NR4A1 Antagonis

9、ts Inhibit 1-Integrin-Dependent Breast Cancer Cell Migration. Mol Cell Biol. 2016 Apr 15;36(9):1383-94.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792;Fax:E-mail: techMedChemE3/2 Master of Small Molecules 您边的抑制剂师

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