1. Vitamin D Related/Nuclear Receptor
  2. Androgen Receptor
  3. Dimethylcurcumin

Dimethylcurcumin  (Synonyms: ASC-J9; GO-Y025)

目录号: HY-15194 纯度: 98.06%
COA 产品使用指南

Dimethylcurcumin (ASC-J9) 是一种雄激素受体降解增强剂,可有效抑制耐药性前列腺癌细胞增殖和侵袭。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Dimethylcurcumin Chemical Structure

Dimethylcurcumin Chemical Structure

CAS No. : 52328-98-0

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥594
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5 mg ¥540
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10 mg ¥900
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25 mg ¥1980
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50 mg ¥3240
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100 mg ¥5220
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500 mg   询价  

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Customer Review

    Dimethylcurcumin purchased from MCE. Usage Cited in: J Ovarian Res. 2018 May 2;11(1):36.  [Abstract]

    Oct4 and Sox2 expression in the GFP (+) cells clearly increased under DHT treatment compared with ASC-J9 treatment based on western blot analysis, which is also consistent with the Nanog expression trend.

    Dimethylcurcumin purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Nov 17;506(1):130-136.  [Abstract]

    The protein expression level of AR in EAM mice with/without ASC-J9 treatment is analysed.

    Dimethylcurcumin purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Nov 17;506(1):130-136.  [Abstract]

    Treatment with ASC-J9 in the presence of TGF-b decreases the mRNA expression of collagen I and a-SMA.

    Dimethylcurcumin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2017 Sep 15;140:73-88.  [Abstract]

    Androgen receptors levels in RAW264.7 cells treated with ASC-J9. Cells are treated with or without ASC-J9 for 30 min or 12 h and cells lysate is examined by western blotting using antibodies for the Androgen Receptor and GAPDH.

    Dimethylcurcumin purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2017 Apr 15;485(4):746-752.  [Abstract]

    ASC-J9 inhibits M1 polarization of Raw264.7 cells. (A) Western blotting and analysis of iNOS in Raw264.7 cells stimulated with LPS in each group. (B) Western blotting and analysis of SOCS1 and p-STAT5 expression in Raw264.7 cells stimulated with LPS in each group.

    Dimethylcurcumin purchased from MCE. Usage Cited in: Oncotarget. 2016 Jun 14;7(24):36814-36828.  [Abstract]

    Protein levels of AR and NANOG expression is measured in NanogPos and NanogNeg cells from T1224+1 and Huh7+7 after treatment with DHT and with or without ASC-J9 for 24h. The addition of ASC-J9 attenuates the DHT effect and reduces the expression of AR and Nanog in both groups.

    Dimethylcurcumin purchased from MCE. Usage Cited in: Tumour Biol. 2015 Nov;36(11):8727-33.  [Abstract]

    Application of ASC-J9 (an AR degradation enhancer) to 22Rv1 cell line also represses androgen-induced Gabarapl1 upregulation.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    > 40 μM
    Compound: 3
    Inhibition of TNF-alpha-induced NFkappaB nuclear translocation in human A549 cells preincubated for 30 mins before TNFalpha challenge and measured 30 post TNFalpha challenge by fluorescence method
    Inhibition of TNF-alpha-induced NFkappaB nuclear translocation in human A549 cells preincubated for 30 mins before TNFalpha challenge and measured 30 post TNFalpha challenge by fluorescence method
    [PMID: 21070043]
    A549 GI50
    5.8 μM
    Compound: 3
    Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay
    [PMID: 21070043]
    HCT-116 GI50
    2 μM
    Compound: GO-Y025
    Growth inhibition of human HCT116 cells after 48 hrs by MTS assay
    Growth inhibition of human HCT116 cells after 48 hrs by MTS assay
    [PMID: 20060305]
    HEK293 EC50
    8.3 μM
    Compound: 1b
    Inhibition of Wnt3A/beta-catenin signaling in HEK293 cells after 24 hrs by firefly/renilla dual luciferase reporter gene assay
    Inhibition of Wnt3A/beta-catenin signaling in HEK293 cells after 24 hrs by firefly/renilla dual luciferase reporter gene assay
    [PMID: 24275249]
    KB CC50
    2 μM
    Compound: 11a
    Compound concentration required to reduce the exponential growth of KB cells by 50%
    Compound concentration required to reduce the exponential growth of KB cells by 50%
    [PMID: 9767632]
    LNCaP IC50
    1.3 μM
    Compound: 71, JC-9, ASC-J9
    Cytotoxicity against human LNCAP cells after 2 days
    Cytotoxicity against human LNCAP cells after 2 days
    [PMID: 20187635]
    LNCaP IC50
    15.3 μM
    Compound: 21
    Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay
    Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay
    [PMID: 22672984]
    LNCaP IC50
    3.9 μM
    Compound: 6
    Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay
    Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay
    [PMID: 19249204]
    MCF-10A IC50
    31.5 μM
    Compound: 6
    Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay
    Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay
    [PMID: 19249204]
    MCF7 IC50
    5.4 μM
    Compound: 6
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    [PMID: 19249204]
    MDA-MB-231 IC50
    4.9 μM
    Compound: 6
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
    [PMID: 19249204]
    MT4 CC50
    4.1 μM
    Compound: 11a
    Compound concentration required to reduce the exponential growth of MT-4 cells by 50%
    Compound concentration required to reduce the exponential growth of MT-4 cells by 50%
    [PMID: 9767632]
    PC-3 IC50
    1.1 μM
    Compound: 71, JC-9, ASC-J9
    Cytotoxicity against human PC3 cells after 2 days
    Cytotoxicity against human PC3 cells after 2 days
    [PMID: 20187635]
    PC-3 IC50
    23.7 μM
    Compound: 21
    Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay
    Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay
    [PMID: 22672984]
    PC-3 IC50
    5.9 μM
    Compound: 6
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    [PMID: 19249204]
    SK-OV-3 IC50
    3.51 μM
    Compound: 15
    Cytotoxicity against human SKOV3 Cells after 48 hrs by Cell Titer Blue assay
    Cytotoxicity against human SKOV3 Cells after 48 hrs by Cell Titer Blue assay
    [PMID: 31129455]
    体外研究
    (In Vitro)

    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[1]. 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[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    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[1]. 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[2]. ASC-J9-treated mice show significantly smaller prostate tumor sizes when compared with those receiving classic ADT/castration with little serum androgen[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    396.43

    Formula

    C23H24O6

    CAS 号
    性状

    固体

    颜色

    Yellow to orange

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : ≥ 50 mg/mL (126.13 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5225 mL 12.6126 mL 25.2251 mL
    5 mM 0.5045 mL 2.5225 mL 5.0450 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.17 mg/mL (5.47 mM); 澄清溶液

      此方案可获得 ≥ 2.17 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 98.06%

    参考文献
    Cell Assay
    [2]

    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 vehicle, 5 μM Dimethylcurcumin (ASC-J9) or 10 μM Dimethylcurcumin (ASC-J9), along with 1 nM DHT, and determined cell viability using Trypan blue staining at specific time intervals.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    CWR22Rv1 cells (1×106 cells per site) are injected into both anterior prostates of castrated nude mouse after 2 weeks of implantation. The mice are randomLy divided into two groups (four mice/eight tumors each group) and either receives 75 mg/kg Dimethylcurcumin (ASC-J9) 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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5225 mL 12.6126 mL 25.2251 mL 63.0628 mL
    5 mM 0.5045 mL 2.5225 mL 5.0450 mL 12.6126 mL
    10 mM 0.2523 mL 1.2613 mL 2.5225 mL 6.3063 mL
    15 mM 0.1682 mL 0.8408 mL 1.6817 mL 4.2042 mL
    20 mM 0.1261 mL 0.6306 mL 1.2613 mL 3.1531 mL
    25 mM 0.1009 mL 0.5045 mL 1.0090 mL 2.5225 mL
    30 mM 0.0841 mL 0.4204 mL 0.8408 mL 2.1021 mL
    40 mM 0.0631 mL 0.3153 mL 0.6306 mL 1.5766 mL
    50 mM 0.0505 mL 0.2523 mL 0.5045 mL 1.2613 mL
    60 mM 0.0420 mL 0.2102 mL 0.4204 mL 1.0510 mL
    80 mM 0.0315 mL 0.1577 mL 0.3153 mL 0.7883 mL
    100 mM 0.0252 mL 0.1261 mL 0.2523 mL 0.6306 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    Dimethylcurcumin
    目录号:
    HY-15194
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