2. STAT3-IN-1

STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis.

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STAT3-IN-1 Chemical Structure

STAT3-IN-1 Chemical Structure

CAS No. : 2059952-75-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 9 publication(s) in Google Scholar

STAT3-IN-1 Related Antibodies

Top Publications Citing Use of Products

    STAT3-IN-1 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2023, 114: 109561.

    STAT3-IN-1 (5 µM) attenuates PA-induced degradation of endothelial TJs by inhibiting phosphorylation of STAT3 in HUVECs.

    • Biological Activity

    • Purity & Documentation

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    Description

    STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis[1].

    IC50 & Target

    IC50: 1.82 μM (STAT3 in HT29 cells), 2.14 μM (STAT3 in MDA-MB 231 cells)[1].
    In Vitro

    STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) inhibits the STAT3 acetylation at lysine 685 and affected its specific genes expressions[1].
    ? STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) induces tumor cells apoptosis in MDA-MB-231 cells[1].

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

    STAT3-IN-1 Related Antibodies

    Apoptosis Analysis[1]

    Cell Line: MDA-MB-231 cell lines.
    Concentration: 0-10 μM.
    Incubation Time: 48 hours.
    Result: The induced apoptosis rates (early and late apoptosis) at 1, 2, 5, 8 and 10 μM were 9.0%, 11.2%, 20.9%, 43.3% and 85.2% versus control 3.0%.

    Western Blot Analysis[1]

    Cell Line: MDA-MB-231 and HT-29 cell lines.
    Concentration: 0-10 μM.
    Incubation Time: 48 hours.
    Result: Inhibited STAT3 acetylation and STAT3 tyrosine phosphorylation in MDA-MB-231 cells.
    Increased the expressions of these tumor-suppressor genes (PTPN6 (SHP-1), CDKN2A and DLEC1) which were related to STAT3 acetylation at Lys685.
    In Vivo

    STAT3-IN-1 (compound 7d: 10, 20 mg/kg, two weeks) arrests tumor growth with low toxicity in mouse-xenograft model[1].

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

    Animal Model: Mouse-xenograft model bearing inoculation of mice breast cancer 4T1 cells[1].
    Dosage: 10, 20 mg/kg.
    Administration: Oral administration once every other day for two weeks.
    Result: Arrested tumor growth with no obvious body weight loss.
    Molecular Weight

    475.53

    Formula

    C28H29NO6
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to orange

    SMILES

    COC1=CC(OC)=CC(/C=C/C2=CC=C(NC(/C=C/C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C2)=C1
    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 : 125 mg/mL (262.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1029 mL 10.5146 mL 21.0292 mL
    5 mM 0.4206 mL 2.1029 mL 4.2058 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.

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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: 6.25 mg/mL (13.14 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 6.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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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

    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 2.1029 mL 10.5146 mL 21.0292 mL 52.5729 mL
    5 mM 0.4206 mL 2.1029 mL 4.2058 mL 10.5146 mL
    10 mM 0.2103 mL 1.0515 mL 2.1029 mL 5.2573 mL
    15 mM 0.1402 mL 0.7010 mL 1.4019 mL 3.5049 mL
    20 mM 0.1051 mL 0.5257 mL 1.0515 mL 2.6286 mL
    25 mM 0.0841 mL 0.4206 mL 0.8412 mL 2.1029 mL
    30 mM 0.0701 mL 0.3505 mL 0.7010 mL 1.7524 mL
    40 mM 0.0526 mL 0.2629 mL 0.5257 mL 1.3143 mL
    50 mM 0.0421 mL 0.2103 mL 0.4206 mL 1.0515 mL
    60 mM 0.0350 mL 0.1752 mL 0.3505 mL 0.8762 mL
    80 mM 0.0263 mL 0.1314 mL 0.2629 mL 0.6572 mL
    100 mM 0.0210 mL 0.1051 mL 0.2103 mL 0.5257 mL
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    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.

    Keywords:

    STAT3-IN-12059952-75-7Inhibitorinhibitorinhibit

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