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  2. Stem Cell/Wnt Autophagy
  3. Gli Autophagy
  4. GANT 61

GANT 61 是靶向 Hedgehog /GLi 通路的 Gli1 和 Gli2 抑制劑。

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)

GANT 61 Chemical Structure

GANT 61 Chemical Structure

CAS No. : 500579-04-4

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2.  同一機(jī)構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機(jī)構(gòu)（單位）一年內(nèi)

     可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥767
In-stock
1 mg ￥316
In-stock
5 mg ￥697
In-stock
10 mg ￥1083
In-stock
50 mg ￥4201
In-stock
100 mg   詢價(jià)  
200 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 56 篇科研文獻(xiàn)

WB
IF
Proliferation Assay

    GANT 61 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 28;420:195-207.  [Abstract]

    Shh-Light 2 cells are transfected with Gli1 or Gli2 plasmids and the expression of proteins are analyzed by Western blot. Positive control JQ1, CBC and CBD inhibit Gli1 and Gli2 overexpression induced Gli luciferase activity, GDC-0499 and GANT61 have no effects.

    GANT 61 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 26;9:674.  [Abstract]

    Cyclopamine and GANT61 decrease the level of Gli1 as evidenced by western blot.

    GANT 61 purchased from MCE. Usage Cited in: Cancer Med. 2018 Nov;7(11):5704-5715.  [Abstract]

    The Hh signaling pathway is involved in DHA induced inhibition of cell proliferation. A and B, CCK8 assay of SKOV3 and SKOV3-IP cells is conducted following treatment with purmorphamine, DHA or a combination of DHA and purmorphamine for 48 h. C and D, SKOV3 and SKOV3‐IP cells are treated with GANT61, DHA, or a combination of DHA and GATN61 for 48 h, while controls are treated with DMSO. CCK8 assay is used to analyze cell viability of SKOV3 and SKOV3-IP cells.

    GANT 61 purchased from MCE. Usage Cited in: Chinese Pharmacological Bulletin. 2018, 34(9): 1235-1242.

    Expression of Gli1/2 (A) and DNA damage proteins (B) at OGD 6 h detected by Western blot.

    GANT 61 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Jan 28;385:128-136.  [Abstract]

    GANT61 or SHH siRNA treatment alone moderately increases LC3-II, and LC3-II increased in cells co-treated with R51211 and GANT61 or SHH siRNA.

    GANT 61 purchased from MCE. Usage Cited in: ACS Appl Mater Interfaces. 2017 Dec 13;9(49):42544-42555.  [Abstract]

    ATG101 cross-talk with the hedgehog pathway modulates hypoxia-induced HPAEC cell proliferation and apoptosis. Effects of ssATG101-TNP on the hedgehog pathway. HPAECs are pretreated with ssATG101-TNP and GANT61; then, they are under hypoxia for 24 h.

    GANT 61 purchased from MCE. Usage Cited in: Life Sci. 2017 Dec 15;191:82-89.  [Abstract]

    ORS cells are exposed to 3% oxygen for 48 h in presence or absence of Shh pathway inhibitor cyclopamine (5 μM) or GANT61 (10 μM). Immunofluorescence assay using anti-PCNA antibody is performed to detect the proliferative ORS cells (red). Cell nuclei are counterstained with DAPI (blue).

    GANT 61 purchased from MCE. Usage Cited in: Cancer Sci. 2017 May;108(5):918-930.  [Abstract]

    Effects of E2 and GANT61 on the protein expression levels of GLI1 and GLI2 in MCF-7 cells. The expression levels are measured with a western blotting as described in the Materials and Methods.

    GANT 61 purchased from MCE. Usage Cited in: Breast Cancer. 2017 Sep;24(5):683-693.  [Abstract]

    Effects of GANT61 (0-20μM) on the expression levels of survivin in MDA-MB-231 cells. The cells are treated with the indicated concentrations of GANT61 for two days. The expression levels are tested using western blotting. The deduced molecular weight of surviving is approximately 16 kDa.

    GANT 61 purchased from MCE. Usage Cited in: Birla Institute of Technology, University of Colorado. 2016 Aug.

    Western blot analyses of whole cell lysates (WCLs) collected from MCF7-Ctrl cells cultured in MCF7-Ctrl and Six1 CM for 48 hrs treated with GANT61 or vehicle.

    GANT 61 purchased from MCE. Usage Cited in: Oncotarget. 2015 Nov 3;6(34):36700-12.  [Abstract]

    BE2-M17 NB cells are incubated with GANT-61 (0–40 μM) for 3 days. The cell viability is monitored using an MTS assay. The expression levels of N-myc and INSM1 in the cells treated with 20 μM of GANT-61 is determined by Western blot analysis. Actin is used as a loading control.

    • 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

    GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.

    IC50 & Target

    Gli1/2[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HeLa IC50
    6.83 μM
    Compound: GANT61
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    		[PMID: 29624387]
    IMR-32 GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human IMR32 cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human IMR32 cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    NIH3T3 EC50
    5 μM
    Compound: 4; GANT-61
    Inhibition of Hh signaling pathway in Shh-LIGHT2 incorporated mouse NIH 3T3 cells assessed as downregulation of Gli1 gene expression by luciferase reporter gene assay
    Inhibition of Hh signaling pathway in Shh-LIGHT2 incorporated mouse NIH 3T3 cells assessed as downregulation of Gli1 gene expression by luciferase reporter gene assay
    		[PMID: 26976215]
    Shh Light II IC50
    5 μM
    Compound: 128, GANT61
    Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay
    Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay
    		[PMID: 19309080]
    SH-SY5Y GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human SH-SY5Y cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human SH-SY5Y cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    SK-N-AS GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human SK-N-AS cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human SK-N-AS cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    SK-N-DZ GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human SK-N-DZ cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human SK-N-DZ cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    SK-N-FI GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human SK-N-FI cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human SK-N-FI cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    SK-N-SH GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human SK-N-SH cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human SK-N-SH cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    體外研究
    (In Vitro)

    GANT61 (20 μM) 比靶向 Smo (環(huán)巴胺) 誘導(dǎo)更多的細(xì)胞死亡。GANT61 (0，5，10，20 μM) 抑制人結(jié)腸癌細(xì)胞系的克隆形成存活。GANT61 (20 μM，0-72 小時(shí)) 下調(diào) HT29 細(xì)胞中的 Gli1 和 Gli2 表達(dá)。GANT61 (0、10 μM 或 20 μM) 差異調(diào)節(jié)參與細(xì)胞死亡和細(xì)胞存活之間平衡的基因[1]。
    GANT-61 抑制細(xì)胞活力并誘導(dǎo)胰腺 CSC 細(xì)胞凋亡。GANT-61 抑制 Shh 通路下游靶標(biāo)的表達(dá)，降低胰腺 CSC 中的 Gli-DNA 相互作用、Gli 轉(zhuǎn)錄活性和 Gli 核轉(zhuǎn)位。GANT-61 差異調(diào)節(jié)參與細(xì)胞存活、細(xì)胞死亡和多能性的基因。GANT-61 抑制 CSCs 的運(yùn)動(dòng)、侵襲和遷移[2]。
    在測(cè)試的神經(jīng)母細(xì)胞瘤細(xì)胞系中，GANT61 敏感性與 GLI1 呈正相關(guān)，與 MYCN 表達(dá)呈負(fù)相關(guān)。GANT61 下調(diào) GLI1、c-MYC、MYCN 和 Cyclin D1 的表達(dá)并誘導(dǎo)神經(jīng)母細(xì)胞瘤細(xì)胞凋亡[3]。

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

    GANT-61 (40 mg/kg，腹腔注射，每周三天) 抑制 NOD/SCID IL2Rγ 缺失小鼠的 CSC 腫瘤生長(zhǎng)[2]。
    GANT61 (50 mg/kg，口服) 以相加或協(xié)同的方式增強(qiáng)用于處理神經(jīng)母細(xì)胞瘤的化療藥物的作用，并減少裸鼠體內(nèi)已建立的神經(jīng)母細(xì)胞瘤異種移植物的生長(zhǎng)[3]。

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

    429.60

    Formula

    C27H35N5
    CAS 號(hào)
    性狀

    固體

    顏色

    White to light yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    Ethanol 中的溶解度 : 66.67 mg/mL (155.19 mM; 超聲助溶)

    DMSO 中的溶解度 : 25 mg/mL (58.19 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.3277 mL 11.6387 mL 23.2775 mL
    5 mM 0.4655 mL 2.3277 mL 4.6555 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)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(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(qǐng)依序添加每種溶劑： 10% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (11.64 mM); 澄清溶液

      此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 EtOH 儲(chǔ)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。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: 5 mg/mL (11.64 mM); 懸濁液; 超聲助溶

      此方案可獲得 5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 EtOH 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)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(chǔ)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(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)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: 99.66%

    參考文獻(xiàn)
    Cell Assay
    [2]

    Cells (1.5×104) are incubated with 0, 1, 5 and 10 μM of GANT-61 in 250 μL of culture medium in 96-well plate for 48 and 72 h. Cell viability is determined by the XTT assay. In brief, a freshly prepared XTT-PMS labeling mixture (50 μL) is added to the cell culture. The absorbance is measured at 450 nm with λ correction at 650 nm. The cell viability is expressed as ΔOD (OD450?? OD650). The apoptosis is determined by FACS analysis of propidium iodide (PI)-stained cells. In brief, cells are trypsinized, washed with PBS and resuspended in 200 μL PBS with 10 μL RNAase (10 mg/mL) and incubated at 37°C for 30 min. After incubation, 50 μL PI solution is added and cells are analyzed for apoptosis using a flow cytometry.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Humanized NOD/SCID/IL2Rgammanull?mice are used for the assay. Before CSC’s injection, mice are humanized with tail vein injection of human normal CD34+?peripheral blood stem/progenitor cells. CD34+peripheral blood stem/progenitor cells (500 cells/mouse, 50-75 μL volume) are injected through tail vein. After 3 days, human pancreatic CSCs (1×103?cells mixed with Matrigel, Becton Dickinson, Bedford, MA, in 75 μL total volume, 50:50 ratio) are injected subcutaneously into the flanks of NOD/SCID IL2Rγnull?mice (4–6 weeks old). After two weeks of CSC implantation, mice (10 mice per group) are treated with GANT-61(0 and 40 mg/kg body weight) ip three times per week for 6 weeks. At the end of the experiment, mice are euthanized, and tumors are isolated for biochemical analysis.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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 / Ethanol 1 mM 2.3277 mL 11.6387 mL 23.2775 mL 58.1937 mL
    5 mM 0.4655 mL 2.3277 mL 4.6555 mL 11.6387 mL
    10 mM 0.2328 mL 1.1639 mL 2.3277 mL 5.8194 mL
    15 mM 0.1552 mL 0.7759 mL 1.5518 mL 3.8796 mL
    20 mM 0.1164 mL 0.5819 mL 1.1639 mL 2.9097 mL
    25 mM 0.0931 mL 0.4655 mL 0.9311 mL 2.3277 mL
    30 mM 0.0776 mL 0.3880 mL 0.7759 mL 1.9398 mL
    40 mM 0.0582 mL 0.2910 mL 0.5819 mL 1.4548 mL
    50 mM 0.0466 mL 0.2328 mL 0.4655 mL 1.1639 mL
    Ethanol 60 mM 0.0388 mL 0.1940 mL 0.3880 mL 0.9699 mL
    80 mM 0.0291 mL 0.1455 mL 0.2910 mL 0.7274 mL
    100 mM 0.0233 mL 0.1164 mL 0.2328 mL 0.5819 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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    Inquiry Information

    產(chǎn)品名稱：
    GANT 61
    目錄號(hào)：
    HY-13901
    需求量：