4(二(1H-吲哚-3-基)甲基)苯酚
- CAS号:151358-47-3
- 英文名:4-(di(1H-indol-3-yl)Methyl)phenol
- 中文名:4(二(1H-吲哚-3-基)甲基)苯酚
- CBNumber:CB12682261
- 分子式:C23H18N2O
- 分子量:338.4
- MOL File:151358-47-3.mol
- 熔点 :122-124 °C
- 沸点 :610.2±50.0 °C(Predicted)
- 密度 :1.321±0.06 g/cm3(Predicted)
- 储存条件 :Sealed in dry,Room Temperature
- 溶解度 :Soluble in DMSO (35 mg/ml); ethanol (35 mg/ml)
- 形态 :solid
- 酸度系数(pKa) :9.98±0.26(Predicted)
- 颜色 :Pink
- 稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
4(二(1H-吲哚-3-基)甲基)苯酚性质、用途与生产工艺
- 生物活性 DIM-C-pPhOH (C-DIM8, CDIM8)是一种 nuclear receptor 4A1 (NR4A1)(Nur77) 拮抗剂。DIM-C-pPhOH 可抑制肿瘤生长和mTOR信号传导，并诱导细胞凋亡和细胞应激。DIM-C-pPhOH 可降低细胞增殖，其对 ACHN细胞 和 786-O细胞 的IC50值分别为13.6 μM 和 13.0 μM。
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靶点
Target Value Nur77
(786-O cells based assay)13.0 μM Nur77
(ACHN cells based assay)13.6 μM -
体外研究
DIM-C-pPhOH (7.5-20 μM; 24 hours; ACHN and 786-O cells) treatment significantly decreases cell proliferation.
DIM-C-pPhOH (20 μM; 24 hours; ACHN and 786-O cells) treatment induces Annexin V staining in ACHN and 786-O cells, confirming that DIM-C-pPhOH induce apoptosis, and also induces cleavage of caspases 7 and 8.
DIM-C-pPhOH (15-20 μM; 24 hours; ACHN and 786-O cells) treatment inhibits NR4A1-regulated expression of survivin, bcl-2 and EGFR in ACHN and 786-O cells. And also induces sestrin 2, activates AMPKα and inhibits activation of mTOR and downstream kinases.
DIM-C-pPhOH decreases expression of β1-integrin protein and mRNA and β1-integrin-dependent responses in MCF7, MDA-MB-231, and SKBR3 cells and also inhibits migration of the latter two cell lines.Cell Proliferation Assay
Cell Line: ACHN and 786-O cells Concentration: 7.5 μM, 15 μM, 20 μM Incubation Time: 24 hours Result: Significantly decreased cell proliferation. Apoptosis Analysis
Cell Line: ACHN and 786-O cells Concentration: 20 μM Incubation Time: 24 hours Result: Induced apoptosis in ACHN and 786-O cells. Western Blot Analysis
Cell Line: ACHN and 786-O cells Concentration: 15 μM, 20 μM Incubation Time: 24 hours Result: Inhibited NR4A1-regulated expression of survivin, bcl-2 and EGFR in ACHN and 786-O cells. And also induced sestrin 2, activated AMPKα and inhibited activation of mTOR and downstream kinases. -
体内研究
DIM-C-pPhOH (30 mg/kg; oral gavage; daily; for 50 days; male athymic nude mice) treatment results in a significant inhibition of tumor growth.
Animal Model: Male athymic nude mice (aged 6-7 weeks) injected with ACHN cells Dosage: 30 mg/kg/day Administration: Oral gavage; daily; for 50 days Result: Resulted in a significant inhibition of tumor growth.
- 更新日期：2024/11/08
- 产品编号：HY-112055
- 产品名称：4(二(1H-吲哚-3-基)甲基)苯酚 DIM-C-pPhOH
- CAS编号：151358-47-3
- 包装：1mg
- 价格：500元
- 更新日期：2024/11/08
- 产品编号：HY-112055
- 产品名称：4(二(1H-吲哚-3-基)甲基)苯酚 DIM-C-pPhOH
- CAS编号：151358-47-3
- 包装：5mg
- 价格：750元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
