二甲基姜黄素

中文名称:

二甲基姜黄素

中文同义词:

ASC-J9 生产厂家;二甲基姜黄素;四甲基姜黄素;二甲基姜黄素, ≥95%

英文名称:

ASC-J9

英文同义词:

1,4,6-Heptatrien-3-one, 1,7-bis(3,4-diMethoxyphenyl)-5-hydroxy-,(1E,4Z,6E)-;(1E,4Z,6E)-1,7-Bis(3,4-dimethoxyphenyl)-5-hydroxy-1,4,6-heptatrien-3-one (ASC-J9);(1E,4Z,6E)-1,7-Bis(3,4-dimethoxyphenyl)-5-hydroxy-1,4,6-heptatrien-3-one;Dimethylcurcumin;GO-Y 025;Dimethylcurcumin, ≥95%;Dimethylcurcumin【(1E,4Z,6E)-1,7-Bis(3,4-dimethoxyphenyl)-5-hydroxy-1,4,6-heptatrien-3-one】

CAS号:

52328-98-0

分子式:

C23H24O6

分子量:

396.43

EINECS号:

2017-001-1

相关类别:

分析试剂标准品;标准品;对照品;中药对照品;植物提取物;对照品-中药对照品;标准品 -中药标准品

Mol文件:

52328-98-0.mol

熔点 

129-130℃

沸点 

588.6±50.0 °C(Predicted)

密度 

1.191

酸度系数(pKa)

8.34±0.60(Predicted)

生物活性

Dimethylcurcumin (ASC-J9, Dimethyl curcumin, GO-Y025)是一种 androgen receptor (AR) 降解促进剂，可通过降解全长和剪接变异体的雄激素受体来抑制去势抵抗性前列腺癌的生长。

靶点

Target Value AR ()

Target

Value

AR ()

体外研究

Dimethylcurcumin (ASC-J9) is able to degrade fAR and AR3 in a dose-dependent manner in various human PCa cells. Dimethylcurcumin (ASC-J9) can also effectively suppress AR-targeted genes in CWR22Rv1-fARKD cells. Dimethylcurcumin (ASC-J9) (5 or 10 µM) significantly suppresses the DHT-induced cell growth in all three PCa cell lines. Dimethylcurcumin (ASC-J9) suppresses AR-targeted genes and cell growth by degradation of fAR and ectopic AR3 in C81 and C4-2 cells. Dimethylcurcumin (ASC-J9) selectively promotes AR degradation by disrupting the interaction between AR and AR coregulators. ASC-J9 reduces the AR aggregated AR-112Q in cells. Dimethylcurcumin (ASC-J9) suppresses the aggregation of AR-112Q in SBMA PC12/AR-112Q cells.

体内研究

Dimethylcurcumin (ASC-J9) (75 mg/kg, i.p.) degrades both fAR and AR3 in the xenografted tumors in vivo, and SC-J9-treated tumors has significantly decreased Ki67-positive cells. Dimethylcurcumin (ASC-J9) (50 mg/kg every 48 h, i.p.) substantially ameliorates the SBMA symptoms in AR-97Q mice, and ameliorates neuromuscular pathological findings. The Dimethylcurcumin (ASC-J9)-treated SBMA mice have relatively normal serum testosterone concentrations. ASC-J9-treated mice show significantly smaller prostate tumor sizes when compared with those receiving classic ADT/castration with little serum androgen.

化学性质 

可溶于甲醇、乙醇、DMSO等有机溶剂。