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  1. Stem Cell/Wnt Metabolic Enzyme/Protease
  2. Hedgehog Smo Endogenous Metabolite
  3. Cyclopamine

Cyclopamine  (Synonyms: 環(huán)巴胺; 11-Deoxojervine)

目錄號(hào): HY-17024 純度: 99.97%
COA 產(chǎn)品使用指南

Cyclopamine 是 Hedgehog 通路的拮抗劑,在細(xì)胞實(shí)驗(yàn)中的 IC50 為 46 nM。Cyclopamine 還是一種選擇性的 Smo 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)

Cyclopamine Chemical Structure

Cyclopamine Chemical Structure

CAS No. : 4449-51-8

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10 mM * 1 mL in DMSO ¥543
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10 mg ¥900
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Customer Review

Other Forms of Cyclopamine:

MCE 顧客使用本產(chǎn)品發(fā)表的 40 篇科研文獻(xiàn)

WB
IF

    Cyclopamine purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Sep 12;10(9):681.  [Abstract]

    Endometrial stromal cells are stimulated with 10 ng/mL TGFβ1 for 48 h. Then these cells are treated with 10 μM Cyc for 24 h and/or cocultured with 10 ng/mL VEGF165 for another 12 or 24 h. The protein levels of collagen 1, α-SMA and smad7 are examined.

    Cyclopamine purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Sep 12;10(9):681.  [Abstract]

    Endometrial stromal cells are stimulated with 10 ng/mL TGFβ1 for 48 h. Then these cells are treated with 10 μM Cyc for 24 h and/or cocultured with 10 ng/mL VEGF165 for another 12 or 24 h. The protein levels of collagen 1, α-SMA and smad7 are examined.

    Cyclopamine 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.

    Cyclopamine purchased from MCE. Usage Cited in: Int J Nanomedicine. 2017 Apr 20;12:3267-3280.  [Abstract]

    The Smo inhibitor Cyclopamine suppresses the activity of Hedgehog–Gli1 signaling. The gene expression and protein production of Smo in MG63 osteoblasts after 7 days of incubation on the different titanium surfaces.

    Cyclopamine 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).

    Cyclopamine purchased from MCE. Usage Cited in: Neurochem Res. 2016 Apr;41(4):687-95.  [Abstract]

    Western blot and RT-qPCR assays of BDNF protein and gene expressions in primary cortical neurons in different experimental conditions. Immunoblotting bands of BDNF protein.
    • 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

    Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.

    IC50 & Target

    Human Endogenous Metabolite

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    49 μM
    Compound: 1
    Anticancer activity against human A549 cells by MTS assay
    Anticancer activity against human A549 cells by MTS assay
    [PMID: 18221872]
    C3H 10T1/2 EC50
    0.17 μM
    Compound: 1
    Inhibition of Hedgehog pathway-dependent oxysterol-induced mouse C3 H10T1/2 cell differentiation assessed as alkaline phosphatase production after 72 hrs
    Inhibition of Hedgehog pathway-dependent oxysterol-induced mouse C3 H10T1/2 cell differentiation assessed as alkaline phosphatase production after 72 hrs
    [PMID: 18842035]
    C3H 10T1/2 IC50
    0.6 μM
    Compound: cyclopamine
    Inhibition of human Shh-induced mouse C3H10T1/2 cell differentiation after 48 hrs by alkaline phosphatase reporter assay
    Inhibition of human Shh-induced mouse C3H10T1/2 cell differentiation after 48 hrs by alkaline phosphatase reporter assay
    [PMID: 23074541]
    C3H 10T1/2 IC50
    0.6 μM
    Compound: Cyclopamine
    Inhibition of N-terminal SHH activated pathway in mouse C3H10T1/2 cells assessed as SAG-induced cell differentiation by alkaline phosphatase assay
    Inhibition of N-terminal SHH activated pathway in mouse C3H10T1/2 cells assessed as SAG-induced cell differentiation by alkaline phosphatase assay
    [PMID: 21592788]
    C3H 10T1/2 IC50
    0.62 μM
    Compound: Cyclopamine
    Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
    Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
    [PMID: 22268551]
    CHO IC50
    1200 nM
    Compound: cyclopamine
    Antagonist activity at mouse Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay
    Antagonist activity at mouse Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay
    [PMID: 19091559]
    CHO IC50
    280 nM
    Compound: cyclopamine
    Antagonist activity at human Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay
    Antagonist activity at human Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay
    [PMID: 19091559]
    Daoy IC50
    0.16 μM
    Compound: 2, Cyc
    Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis
    Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis
    [PMID: 24900716]
    HEK293 IC50
    64 nM
    Compound: Cyclopamine
    Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
    Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
    [PMID: 22268551]
    Medulloblastoma cell EC50
    1 μM
    Compound: 16
    Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
    Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
    [PMID: 17417631]
    MEF IC50
    1.9 μM
    Compound: cyclopamine
    Inhibition of Smo in mouse Ptch-deficient MEF cells assessed as inhibition of Shh-induced Gli-responsive betagalactosidase activity after 30 hrs by BetaGLo assay
    Inhibition of Smo in mouse Ptch-deficient MEF cells assessed as inhibition of Shh-induced Gli-responsive betagalactosidase activity after 30 hrs by BetaGLo assay
    [PMID: 23074541]
    Shh Light II IC50
    0.3 μM
    Compound: Cyclopamine
    Inhibition of SHH pathway in mouse Shh Light2 cells after 40 hrs by Gli-dependent luciferase reporter gene assay
    Inhibition of SHH pathway in mouse Shh Light2 cells after 40 hrs by Gli-dependent luciferase reporter gene assay
    [PMID: 21592788]
    Shh Light II IC50
    0.3 μM
    Compound: Cyclopamine
    Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
    Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
    [PMID: 22268551]
    Shh Light II IC50
    1312 nM
    Compound: Cyclopamine
    Inhibition of SHH in mouse Shh-Light2 cells after 48 hrs by Gli1 reporter gene assay in presence of SAG
    Inhibition of SHH in mouse Shh-Light2 cells after 48 hrs by Gli1 reporter gene assay in presence of SAG
    [PMID: 19541490]
    Shh Light II IC50
    484 nM
    Compound: Cyc
    Antagonist activity at Smo in mouse Shh-Light 2 cells assessed as inhibition of Shh-induced Gli1-reporter activity after 2 days by dual-luciferase reporter gene method
    Antagonist activity at Smo in mouse Shh-Light 2 cells assessed as inhibition of Shh-induced Gli1-reporter activity after 2 days by dual-luciferase reporter gene method
    [PMID: 23063522]
    Shh Light II EC50
    500 nM
    Compound: 3
    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]
    TM3 IC50
    46 nM
    Compound: cyclopamine
    Inhibition of Hedgehog signaling pathway in mouse TM3 cells bearing pTA-8xGli-Luc reporter construct assessed as transcriptional modulation of Gli after 48 hrs by luciferase assay
    Inhibition of Hedgehog signaling pathway in mouse TM3 cells bearing pTA-8xGli-Luc reporter construct assessed as transcriptional modulation of Gli after 48 hrs by luciferase assay
    [PMID: 19091559]
    U-87MG ATCC IC50
    22.5 μM
    Compound: Cyc
    Antiproliferative activity against human U87MG cells after 72 hrs by MTS assay
    Antiproliferative activity against human U87MG cells after 72 hrs by MTS assay
    [PMID: 22226657]
    體外研究
    (In Vitro)

    Treatment with small molecule Hh inhibitors such as HhAntag and the natural product Cyclopamine, both binding to Smo, induces tumor remission in a genetic mouse model of medulloblastoma[1]. Cyclopamine is a Hedgehog (Hh) pathway antagonist. Cyclopamine suppresses cell growth. Cyclopamine (3 μM) suppression of Hh pathway activity and growth in digestive tract tumour cell lines correlates with expression of PTCHmRNA[2]. Cyclopamine is a steroidal alkaloid that inhibits Hh signalling through direct interaction with Smo[3].

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

    體內(nèi)研究
    (In Vivo)

    Cyclopamine causes durable regression of xenograft tumors. Tumors in Cyclopamine-treated animals, regress completely by 12 days[2]. Cyclopamine (1.2 mg) treatment blocks tumour formation of human pancreatic adenocarcinoma cells after transplantation into nude mice[3].

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

    分子量

    411.62

    Formula

    C27H41NO2

    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    環(huán)杷明;環(huán)巴胺;11-去氧芥芬胺

    結(jié)構(gòu)分類
    初始來源
    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 : 20 mg/mL (48.59 mM; 超聲助溶)

    DMSO 中的溶解度 : 10 mg/mL (24.29 mM; 超聲助溶 (<80°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.4294 mL 12.1471 mL 24.2943 mL
    5 mM 0.4859 mL 2.4294 mL 4.8589 mL
    查看完整儲(chǔ)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(chǔ)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(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?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請?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

      請依序添加每種溶劑: 10% EtOH    90% Corn Oil

      Solubility: ≥ 1.67 mg/mL (4.06 mM); 澄清溶液

      此方案可獲得 ≥ 1.67 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

      1 mL 工作液為例,取 100 μL 16.7 mg/mL 的澄清 EtOH 儲(chǔ)備液加到 900 μL 玉米油中,混合均勻。

    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% Corn Oil

      Solubility: ≥ 1 mg/mL (2.43 mM); 澄清溶液

      此方案可獲得 ≥ 1 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

      1 mL 工作液為例,取 100 μL 10.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

    動(dòng)物溶解方案計(jì)算器
    請輸入動(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

    由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
    請輸入您的動(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(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,請謹(jǐn)慎選擇該方案。
    請確保第一步儲(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: 99.97%

    參考文獻(xiàn)
    Cell Assay
    [2]

    Cells are cultured in triplicate in 96-well plates in assay media to which 5E1 monoclonal antibody, ShhNp and/or Cyclopamine (3 μM) are added at 0 h at concentrations indicated in the main text. Viable cell mass is determined by optical density measurements at 490 nm (OD490) at 2 and 4 days using the CellTiter96 colorimetric assay. Relative growth is calculated as OD (day 4)-OD (day 2)/OD (day 2)[2].

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

    Animal Administration
    [3]

    Mice[3]
    A total of 0.1 mL Hanks’ balanced salt solution and matrigel (1:1) containing 2×106 cells is injected subcutaneously into CD-1 nude mice. Tumors are grown for 4 days to a minimum volume of 125 mm3; treatment is initiated simultaneously for all subjects. Mice are injected subcutaneously with vector alone (triolein:ethanol 4:1 v/v) or a Cyclopamine suspension (1.2 mg per mouse in triolein:ethanol 4:1 v/v) daily for 7 days. At the end of the treatment period, tumours are excised from mice, weighed and then fixed for 3 h at 4°C with 4% paraformaldehyde, embedded in paraffin wax and sectioned (6 μm). Apoptotic cells are identified by TUNEL using recombinant Tdt. Sections are then counterstained with eosin. Eight ×20-magnified fields from regions corresponding to the exterior, middle and interior of two control and two cyclopamine-treated tumours are chosen at random. We counted the number of TUNEL-positive nuclei manually. Haematoxylin/eosin staining is done.

    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?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請?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 2.4294 mL 12.1471 mL 24.2943 mL 60.7356 mL
    5 mM 0.4859 mL 2.4294 mL 4.8589 mL 12.1471 mL
    10 mM 0.2429 mL 1.2147 mL 2.4294 mL 6.0736 mL
    15 mM 0.1620 mL 0.8098 mL 1.6196 mL 4.0490 mL
    20 mM 0.1215 mL 0.6074 mL 1.2147 mL 3.0368 mL
    Ethanol 25 mM 0.0972 mL 0.4859 mL 0.9718 mL 2.4294 mL
    30 mM 0.0810 mL 0.4049 mL 0.8098 mL 2.0245 mL
    40 mM 0.0607 mL 0.3037 mL 0.6074 mL 1.5184 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:
    Cyclopamine
    目錄號(hào):
    HY-17024
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