生物活性 | |||
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描述 | Nerve growth factor-induced Bα (Nur77) is an orphan nuclear receptor overexpressed in colon tumors. DIM-C-pPhOCH3 is a Nur77 agonist. It inhibited RKO cell growth at 24-, 48-, and 72-h post-treatment at a concentration of 10μmol/L. PARP cleavage was observed in RKO cells treated with 12.5μmol/L DIM-C-pPhOCH3 for 48 hours. Treatment with 12.5μmol/L DIM-C-pPhOCH3 for 48 hours also induced the expression of TRAIL protein in RKO cells. DIM-C-pPhOCH3 at a concentration of 12.5 μmol/L also induced the gene expression of PDCD1, CSE, and ATF3 in RKO cells 6 hours after exposure. DIM-C-pPhOCH3 treatment at 12.5 μmol/L induced apoptosis (PARP cleavage) in RKO, SW480, HCT-116, and HT-29 cells at 24-h post-treatment but not in HCT-15 cells. In athymic nude mice bearing RKO cell xenografts, oral administration of DIM-C-pPhOCH3 at a dosage of 25 mg/kg/d for 21 days significantly inhibited tumor growth compared with corn oil-treated controls[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.84mL 0.57mL 0.28mL |
14.19mL 2.84mL 1.42mL |
28.37mL 5.67mL 2.84mL |
参考文献 |
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