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  2. JAK/STAT Signaling Stem Cell/Wnt Epigenetics Protein Tyrosine Kinase/RTK
  3. STAT JAK
  4. Cucurbitacin I

Cucurbitacin I  (Synonyms: 葫蘆素 I; Elatericin B; JSI-124; NSC-521777)

目錄號(hào): HY-N1405 純度: 99.44%
COA 產(chǎn)品使用指南 技術(shù)支持

Cucurbitacin I 是 JAK2/STAT3 的天然選擇性抑制劑，并具有有效的抗腫瘤活性。

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)

Cucurbitacin I Chemical Structure

Cucurbitacin I Chemical Structure

CAS No. : 2222-07-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥4280
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1 mg ￥1480
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5 mg ￥3780
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10 mg ￥5650
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50 mg   詢(xún)價(jià)  
100 mg   詢(xún)價(jià)  

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Customer Review

Other Forms of Cucurbitacin I:

    Cucurbitacin I purchased from MCE. Usage Cited in: Cell Cycle. 2019 Nov;18(21):3010-3029.  [Abstract]

    Western blot analysis of C3, NICD, p-Stat3, and Stat3 expression in astrocytes treated with MCM or MCM plus the Stat3 inhibitor JSI-124 (0.2 or 0.5 μM) for 24 h.

    查看 STAT 亞型特異性產(chǎn)品:

    查看 JAK 亞型特異性產(chǎn)品:

    • 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

    Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.

    IC50 & Target

    JAK2

     

    STAT3

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    C8166 EC50
    0.7 μg/mL
    Compound: 7
    Antiviral activity against HIV1 in C8166 cells after 72 hrs
    Antiviral activity against HIV1 in C8166 cells after 72 hrs
    		[PMID: 18088099]
    C8166 CC50
    14.4 μg/mL
    Compound: 7
    Cytotoxicity against human C8166 cells by MTT method
    Cytotoxicity against human C8166 cells by MTT method
    		[PMID: 18088099]
    HepG2 IC50
    15.8 μM
    Compound: 5
    Cytotoxicity against human HepG2 cells after 24 hrs assessed as inhibition of cell viability by MTT assay
    Cytotoxicity against human HepG2 cells after 24 hrs assessed as inhibition of cell viability by MTT assay
    		[PMID: 21459003]
    HepG2 EC50
    3.16 μM
    Compound: 5
    Hepatoprotective activity in human HepG2 cells assessed as inhibition of CCl4-induced toxicity after 24 hrs by MTT assay
    Hepatoprotective activity in human HepG2 cells assessed as inhibition of CCl4-induced toxicity after 24 hrs by MTT assay
    		[PMID: 21459003]
    HL-60 IC50
    0.1 nM
    Compound: 2
    Cytotoxicity against human HL60 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human HL60 cells after 72 hrs by WST-8 assay
    		[PMID: 20347305]
    HSC-T6 EC50
    0.02 μM
    Compound: 5
    Antiproliferative activity against serum-stimulated rat HSC-T6 cells after 24 hrs by MTT assay
    Antiproliferative activity against serum-stimulated rat HSC-T6 cells after 24 hrs by MTT assay
    		[PMID: 21459003]
    HSC-T6 IC50
    3.6 μM
    Compound: 5
    Cytotoxicity against rat HSC-T6 cell after 24 hrs by MTT assay
    Cytotoxicity against rat HSC-T6 cell after 24 hrs by MTT assay
    		[PMID: 21459003]
    HT-1080 IC50
    0.47 nM
    Compound: 2
    Cytotoxicity against human HT1080 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human HT1080 cells after 72 hrs by WST-8 assay
    		[PMID: 20347305]
    HT-29 IC50
    0.19 μM
    Compound: 12
    Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
    Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
    		[PMID: 22239601]
    JY IC50
    0.95 μM
    Compound: 3
    Inhibition of LFA1 expressed in human JY cells interaction with ICAM1-IG expressed in human HeLa cell monolayer after 45 mins by cell adhesion assay
    Inhibition of LFA1 expressed in human JY cells interaction with ICAM1-IG expressed in human HeLa cell monolayer after 45 mins by cell adhesion assay
    		[PMID: 7852999]
    MCF7 IC50
    0.0607 μM
    Compound: 7
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay
    		[PMID: 25756299]
    U-937 IC50
    0.3 nM
    Compound: 2
    Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay
    		[PMID: 20347305]
    體外研究
    (In Vitro)

    Exposure of the COLO205 cells to Cucurbitacin I significantly decreases cell viability. The anticancer activity of Cucurbitacin I is accomplished by downregulating p-STAT3 and MMP-9 expression[1]. PE-induced cell enlargement and upregulation of ANF and β-MHC are significantly suppressed by pretreatment of the cardiomyocytes with Cucurbitacin I. Notably, Cucurbitacin I also impaires connective tissue growth factor (CTGF) and MAPK signaling, pro-hypertrophic factors, as well as TGF-β/Smad signaling, the important contributing factors to fibrosis[2]. Incubation of the Seax cell line with the Jak/Stat3 inhibitor Cucurbitacin I result in a time- and concentration-dependent decrease of P-Stat3 and Stat3. In freshly isolated Sz cells (n=3), Cucurbitacin I induces a concentration-dependent decrease in Stat3 expression whereas P-Stat3 is undetectable. Finally, incubation of freshly isolated Sz cells (n=4) with 30 μM Cucurbitacin I for 6 hours induces apoptosis in the large majority (73-91%) of tumor cells[3].

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

    No major side effects are noted throughout the study. It is shown that average tumor volumes at the end of the study are as follows: control, 616 mm3 (±130); CQ, 580 mm3 (±107); Cucurbitacin I, 346mm3 (±79); and combination, 220mm3 (±62). The differences in tumor volume between the Cucurbitacin I and control, combination and control, and combination and Cucurbitacin I arms are significant. Furthermore, combination-treated tumors exhibit a significantly lower average tumor weight at study termination than the control. Moreover, there was no effect on the body weights of mice[4].

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

    514.65

    Formula

    C30H42O7
    CAS 號(hào)
    性狀

    固體

    顏色

    White to yellow

    中文名稱(chēng)

    葫蘆素 I
    結(jié)構(gòu)分類(lèi)
    初始來(lái)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 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 : ≥ 100 mg/mL (194.31 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.9431 mL 9.7153 mL 19.4307 mL
    5 mM 0.3886 mL 1.9431 mL 3.8861 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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?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(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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 3 mg/mL (5.83 mM); 澄清溶液

      此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 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% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 3 mg/mL (5.83 mM); 澄清溶液

      此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 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(guò)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(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    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(guò)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(guó)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(guò)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: 99.44%

    參考文獻(xiàn)
    Animal Administration
    [4]

    Mice[4]
    BALB/c nude (nu/nu) female mice are used. U251 cells (5×106 cells in 50 μL of serum-free DMEM) are inoculated subcutaneously into the right flank of 5-week-old female mice after acclimatization for a week. Tumor growth is measured daily with calipers. When the tumors reach a mean volume of 90-120 mm3, animals are randomized into groups. In the first experiment, 16 mice are randomly assigned to Cucurbitacin I (1 mg/kg/day in 20% DMSO in PBS) or drug vehicle control (20% DMSO in PBS) and dosed intraperitoneally with 100 μL of vehicle or drug once daily for 18 days, whereas, in the second, 20 mice are assigned to four groups. Control animals receive 20% DMSO in PBS vehicle, whereas treated animals are injected with Cucurbitacin I (1 mg/kg/day) in 20% DMSO in PBS, CQ (25 mg/kg/day) in 20% DMSO in PBS, and Cucurbitacin I (1 mg/kg/day) plus CQ (25 mg/kg/day) in 20% DMSO in PBS and dosed intraperitoneally with 100 μL of vehicle or drug once daily for 15 days[4].

    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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?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 1.9431 mL 9.7153 mL 19.4307 mL 48.5767 mL
    5 mM 0.3886 mL 1.9431 mL 3.8861 mL 9.7153 mL
    10 mM 0.1943 mL 0.9715 mL 1.9431 mL 4.8577 mL
    15 mM 0.1295 mL 0.6477 mL 1.2954 mL 3.2384 mL
    20 mM 0.0972 mL 0.4858 mL 0.9715 mL 2.4288 mL
    25 mM 0.0777 mL 0.3886 mL 0.7772 mL 1.9431 mL
    30 mM 0.0648 mL 0.3238 mL 0.6477 mL 1.6192 mL
    40 mM 0.0486 mL 0.2429 mL 0.4858 mL 1.2144 mL
    50 mM 0.0389 mL 0.1943 mL 0.3886 mL 0.9715 mL
    60 mM 0.0324 mL 0.1619 mL 0.3238 mL 0.8096 mL
    80 mM 0.0243 mL 0.1214 mL 0.2429 mL 0.6072 mL
    100 mM 0.0194 mL 0.0972 mL 0.1943 mL 0.4858 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(chēng)：
    Cucurbitacin I
    目錄號(hào)：
    HY-N1405
    需求量：