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

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

Cat. No.: HY-N1405 Purity: 99.44%
COA Handling Instructions

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

For research use only. We do not sell to patients.

Cucurbitacin I Chemical Structure

Cucurbitacin I Chemical Structure

CAS No. : 2222-07-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 249 In-stock
Solution
10 mM * 1 mL in DMSO USD 249 In-stock
Solid
1 mg USD 95 In-stock
5 mg USD 220 In-stock
10 mg USD 290 In-stock
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Cucurbitacin I:

Top Publications Citing Use of Products

    Cucurbitacin I purchased from MedChemExpress. 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.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    JAK2

     

    STAT3

     

    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].

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

    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].

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

    Molecular Weight

    514.65

    Formula

    C30H42O7

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CC(C)(C1=CC[C@@]2([H])[C@@]3(C[C@@H](O)[C@@H]([C@]3(C4)C)[C@@](C)(O)C(/C=C/C(C)(O)C)=O)C)C(C(O)=C[C@@]1([H])[C@]2(C)C4=O)=O

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (194.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 3 mg/mL (5.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 3 mg/mL (5.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    mg/kg

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.44%

    References
    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.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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