2. JAK/STAT Signaling Stem Cell/Wnt Protein Tyrosine Kinase/RTK Epigenetics
  3. STAT JAK
  4. 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 283 In-stock
Solution
10 mM * 1 mL in DMSO USD 283 In-stock
Solid
1 mg USD 95 In-stock
5 mg USD 250 In-stock
10 mg USD 400 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Cucurbitacin I:

Cucurbitacin I Related Antibodies

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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    JAK1 JAK2 JAK3 Tyk2 JAK

    • 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.

    Cucurbitacin I Related Antibodies
    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

    Appearance

    Solid

    Formula

    C30H42O7
    CAS No.
    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)

    *"≥" 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
    10 mM 0.1943 mL 0.9715 mL 1.9431 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.44%

    COA (253 KB) HNMR (250 KB) LCMS (264 KB)

    Handling Instructions (2659 KB)
    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
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    Cucurbitacin I Related Classifications

    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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    Keywords:

    Cucurbitacin I2222-07-3Elatericin B JSI-124 NSC-521777JSI124JSI 124JSI-124NSC521777NSC 521777NSC-521777STATJAKJanus kinaseInhibitorinhibitorinhibit

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