Product Introduction
Bioactivity


英文名: Dimethylcurcumin

描述: Dimethylcurcumin (ASC-J9) 是雄激素受體降解增強劑，能夠有效抑制耐藥性前列腺癌細胞增殖和侵襲。

細胞實驗: For the cell survival assay, the PC12/AR-112Q and PC12/AR-10Q cells are cultured as described previously and incubated cells in the presence of 10 μg/mL doxycycline for 24 h. Then the cells are treated with a vehicle, 5 μM Dimethylcurcumin or 10 μM Dimethylcurcumin, along with 1 nM DHT, and determined cell viability using Trypan blue staining at specific time intervals [2].

動物實驗: CWR22Rv1 cells (1×10^6 cells per site) are injected into both anterior prostates of the castrated nude mice after 2 weeks of implantation. The mice were randomly divided into two groups (four mice/eight tumors each group) and either receive 75 mg/kg Dimethylcurcumin intraperitoneal injection or vehicle control every other day. After 4 weeks of treatment, all mice are killed to examine the tumor growth. Body weights and mice activity are measured weekly [1].

體外活性: Dimethylcurcumin 在不同的人類前列腺癌細胞中以劑量依賴的方式降解 fAR 和 AR3。在 CWR22Rv1-fARKD 細胞中，Dimethylcurcumin 也能有效地抑制 AR 靶基因。Dimethylcurcumin (5 或 10 μM) 顯著抑制三種前列腺癌細胞線中 DHT 誘導的細胞增長。Dimethylcurcumin 通過降解 C81 和 C4-2 細胞中的 fAR 和異位 AR3 來抑制 AR 靶基因和細胞生長 [1]。ASC-J9 減少細胞中 AR 聚集的 AR-112Q。Dimethylcurcumin 抑制 SBMA PC12/AR-112Q 細胞中的 AR-112Q 聚集 [2]。

體內(nèi)活性: Dimethylcurcumin（75 mg/kg，腹腔注射）能在體內(nèi)降解異種移植腫瘤中的fAR和AR3，并且經(jīng)ASC-J9處理的腫瘤顯示Ki67陽性細胞顯著減少[1]。Dimethylcurcumin（50 mg/kg，每48小時一次，腹腔注射）顯著改善了AR-97Q小鼠的脊髓性肌萎縮癥狀，并改善了神經(jīng)肌肉病理學發(fā)現(xiàn)[2]。與接受經(jīng)典ADT/去勢治療且血清雄激素水平較低的小鼠相比，ASC-J9處理的小鼠展示了顯著更小的前列腺腫瘤體積[3]。

存儲條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 48 mg/mL (121.08 mM)
H2O : Insoluble


關鍵字: Dimethylcurcumin | inhibit | Androgen Receptor | GO-Y 025 | Inhibitor | GO-Y-025

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