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

Dimethylcurcumin  (Synonyms: 二甲基姜黃素; ASC-J9; GO-Y025)

目錄號: HY-15194 純度: 98.06%
COA 產(chǎn)品使用指南 技術(shù)支持

Dimethylcurcumin (ASC-J9) 是一種雄激素受體降解增強(qiáng)劑，可有效抑制耐藥性前列腺癌細(xì)胞增殖和侵襲。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Dimethylcurcumin Chemical Structure

Dimethylcurcumin Chemical Structure

CAS No. : 52328-98-0

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規(guī)格 價(jià)格 是否有貨 數(shù)量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥594
In-stock
5 mg ￥540
In-stock
10 mg ￥900
In-stock
25 mg ￥1980
In-stock
50 mg ￥3240
In-stock
100 mg ￥5220
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

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]

    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 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 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

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

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

    細(xì)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]
    體外研究
    (In Vitro)

    Dimethylcurcumin 能夠在各種人類 PCa 細(xì)胞中以劑量依賴性方式降解 fAR 和 AR3。Dimethylcurcumin 還可以有效抑制 CWR22Rv1-fARKD 細(xì)胞中的 AR 靶向基因。Dimethylcurcumin (5 或 10 μM) 顯著抑制所有三種 PCa 細(xì)胞系中 DHT 誘導(dǎo)的細(xì)胞生長。Dimethylcurcumin 通過降解 C81 和 C4-2 細(xì)胞中的 fAR 和異位 AR3 來抑制 AR 靶向基因和細(xì)胞生長[1]。
    Dimethylcurcumin 通過破壞 AR 和 AR 輔助調(diào)節(jié)劑之間的相互作用，選擇性地促進(jìn) AR 降解。Dimethylcurcumin 減少細(xì)胞中 AR 聚集的 AR-112Q。Dimethylcurcumin 抑制 SBMA PC12/AR-112Q 細(xì)胞中 AR-112Q 的聚集[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    Dimethylcurcumin (75 mg/kg，腹腔注射) 在體內(nèi)降解異種移植腫瘤中的 fAR 和 AR3，并且 SC-J9 處理的腫瘤顯著減少了 Ki67 陽性細(xì)胞[1] 。
    Dimethylcurcumin (50 mg/kg，每 48 小時(shí)一次，腹腔注射) 顯著改善 AR-97Q 小鼠的 SBMA 癥狀，并改善神經(jīng)肌肉病理學(xué)發(fā)現(xiàn)。Dimethylcurcumin 處理的 SBMA 小鼠具有相對正常的血清睪酮濃度[2]。
    與接受經(jīng)典 ADT/閹割且血清雄激素很少的小鼠相比，Dimethylcurcumin 處理的小鼠顯示出顯著更小的前列腺腫瘤[3]。

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

    396.43

    Formula

    C23H24O6
    CAS 號
    性狀

    固體

    顏色

    Yellow to orange

    結(jié)構(gòu)分類
    初始來源
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : ≥ 50 mg/mL (126.13 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實(shí)驗(yàn)：

    請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 2.17 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 21.7 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    動物溶解方案計(jì)算器
    請輸入動物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 98.06%

    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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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    產(chǎn)品名稱：
    Dimethylcurcumin
    目錄號：
    HY-15194
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