4(二(1H-吲哚-3-基)甲基)苯酚

4(二(1H-吲哚-3-基)甲基)苯酚

中文名称4(二(1H-吲哚-3-基)甲基)苯酚
中文同义词4(二(1H-吲哚-3-基)甲基)苯酚;化合物DIM-C-PPHOH;DIM-C-PPHOH,NUR77拮抗剂
英文名称4-(di(1H-indol-3-yl)Methyl)phenol
英文同义词4-(di(1H-indol-3-yl)Methyl)phenol;DIM-C-pPhOH;4-[bis(1H-indol-3-yl)methyl]phenol;C-DIM8;1,1-Bis(3'-indolyl)-1-(p-hydroxyphenyl)methane;DIM-C-pPhOH(CDIM8);Phenol, 4-(di-1H-indol-3-ylmethyl)-;inhibit,receptor,Inhibitor,β1-integrin,mTOR,cancer,DIMCpPhOH,signaling,nuclear,xenografts,Apoptosis,DIM C pPhOH,stress
CAS号151358-47-3
分子式C23H18N2O
分子量338.4
EINECS号
相关类别吲哚类
Mol文件151358-47-3.mol
结构式4(二(1H-吲哚-3-基)甲基)苯酚 结构式

4(二(1H-吲哚-3-基)甲基)苯酚 性质

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
溶解度溶于 DMSO (35 mg/ml);乙醇(35 毫克/毫升)
形态固体
酸度系数(pKa)9.98±0.26(Predicted)
颜色粉色
稳定性自购买之日起 2 年内保持稳定。 DMSO 溶液可在 -20°C 下保存长达 2 个月。

4(二(1H-吲哚-3-基)甲基)苯酚 用途与合成方法

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。
TargetValue
Nur77
(786-O cells based assay)
13.0 μM
Nur77
(ACHN cells based assay)
13.6 μM

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.

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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/08/19HY-1120554(二(1H-吲哚-3-基)甲基)苯酚
DIM-C-pPhOH
151358-47-31mg500元
2024/08/19HY-1120554(二(1H-吲哚-3-基)甲基)苯酚
DIM-C-pPhOH
151358-47-35mg750元

4(二(1H-吲哚-3-基)甲基)苯酚 上下游产品信息

"4(二(1H-吲哚-3-基)甲基)苯酚"相关产品信息
左乙拉西坦 去甲氟西汀 树脂毒素 替加环素 吲哚 2,3,3-三甲基-3H-吲哚 1,3,3-三甲基-2-亚甲基吲哚啉
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