1. JAK/STAT Signaling Stem Cell/Wnt
  2. STAT
  3. NSC 74859

NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC50 of 86 μM.

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

NSC 74859 Chemical Structure

NSC 74859 Chemical Structure

CAS No. : 501919-59-1

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Customer Review

Based on 47 publication(s) in Google Scholar

Top Publications Citing Use of Products

42 Publications Citing Use of MCE NSC 74859

WB

    NSC 74859 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Feb 27;42(1):51.  [Abstract]

    The enhanced phosphorylation level of JAK2 and STAT3 mediated by rhCCL18 can be reversed by NSC 74859 (S3I-201) in EC-109, EC-109 Vector and EC-109 shPITPNM3 cells.

    NSC 74859 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Aug 28;430:201-214.  [Abstract]

    CD146WT or CD146KO MEFs are stimulated with or without TGF-β1 (10 ng/mL) for 24 h in the presence or absence of NSC74859 (200 μM). The expression of CD146, the expression and activation of STAT3, and the expression levels of E-cadherin, N-cadherin, and Twist are assessed by immunoblotting.

    NSC 74859 purchased from MedChemExpress. Usage Cited in: Biofactors. 2018 Nov;44(6):570-576.  [Abstract]

    Westen Blot analysis of HMGB1 expression in HepG2 cells in the treatment of Stat3 inhibitor NSC74859 (SI3), or activator (NAC).

    NSC 74859 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Aug 30.  [Abstract]

    AA-FLS are treated with different concentrations (25, 50, and 100 µM) of Ferulic acid (FA) and 50 µM of S3I-201 and then cultured in the presence or absence of IL-17 (10 ng/mL). The cell lysates are subjected to Western blot analysis to assess the expression levels of TLR-3, Cyr61, IL-23 and GM-CSF proteins.

    NSC 74859 purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2017 Nov;91:134-144.  [Abstract]

    AA-FLS cultured in the presence or absence of S3I-201 for 24 h, then treated with IL-17 for an additional 24 h and phosphorylation of STAT-3 is detected by western blotting.

    View All STAT Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC50 of 86 μM[1].

    IC50 & Target[1]

    STAT3

    86 μM (IC50)

    In Vitro

    NSC 74859 (S3I-201) preferentially inhibits Stat3 DNA-binding activity over that of Stat1 (IC50 values, Stat3•Stat3, 86±33 μM; Stat1•Stat3, 160±43 μM; and Stat1•Stat1, >300 μM) and inhibits that of Stat5 with IC50 of 166±17 μM). NSC 74859 significantly reduces viable cell numbers and inhibits growth of transformed mouse fibroblasts NIH 3T3/v-Src and breast carcinoma cell lines (MDA-MB-231, MDA-MB-435, and MDA-MB-468). At 30-100 μM, NSC 74859 induces significant apoptosis in the representative human breast carcinoma cell line MDA-MB-435 and NIH 3T3/v-Src, both of which harbor constitutively active Stat3. The breast carcinoma MDA-MB-435 cell line is more sensitive to 30 μM NSC 74859. By contrast, the human breast cancer MDA-MB-453 cells and the normal mouse fibroblasts (NIH 3T3), which do not contain abnormal Stat3 activity, are less sensitive to NSC 74859 at 100 μM or less. At 300 μM or higher, NSC 74859 induced general, nonspecific cytotoxicity independent of Stat3 activation status[1]. Huh-7 cells do not express β2SP or TBGFR2 and are sensitive to STAT3 inhibition, with an IC50 of 100 μM for NSC 74859, regardless of CD133+ status. The IC50 of NSC 74859 is 150 μM for Huh-7 and SNU-398 cells, 15 μM for SNU-475 cells and 200 μM for SNU-182 cells. NSC 74859 inhibits breast carcinoma MDA-MB-435, MDA-MB-453 and MDA-MB-231 cell lines with an IC50 close to 100 μM[2].

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

    In Vivo

    Human breast (MDA-MB-231) tumor-bearing mice are given an i.v. injection of NSC 74859 (S3I-201) or vehicle every 2 or every 3 days for 2 weeks, and tumor measurements are taken every 2-3 days. Compared with control (vehicle-treated) tumors, which continued to grow, human breast tumors in mice that received S3I-201 display strong growth inhibition. Continued evaluation of treated mice on termination of treatment shows no resumption of tumor growth, suggesting potentially a long-lasting effect of S3I-201 on tumor growth[1]. Compared with vehicle-treated control tumors (n=15), which continued to grow, S3I-201 treatment of somatotroph tumor xenografts (n=15) significantly attenuated tumor growth for the duration of the experiment. Tumors derived from NSC 74859-treated rats are significantly smaller than those from the untreated group (220±16 mm3 vs. 287±16 mm3, P<0.01) as early as 5 days after NSC 74859 injection. Fifteen days after treatments, the average tumor volume of NSC 74859-treated rats is 64% of that of controls (449±40 mm3 vs. 708±83 mm3, P<0.01). Rats are sacrificed and tumors are harvested 15 days after treatment initiation. The average tumor weight of NSC 74859-treated rats is 78±8 mg, while tumors derived from control rats weighed 114±13 mg (32% reduction; P<0.05)[3].

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

    Molecular Weight

    365.36

    Formula

    C16H15NO7S

    CAS No.
    Appearance

    Solid

    Color

    White to gray

    SMILES

    OC1=CC(NC(COS(=O)(C2=CC=C(C=C2)C)=O)=O)=CC=C1C(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (273.70 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 2.7370 mL 13.6851 mL 27.3703 mL
    5 mM 0.5474 mL 2.7370 mL 5.4741 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 7.5 mg/mL (20.53 mM); Clear solution

      This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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: ≥ 7.5 mg/mL (20.53 mM); Clear solution

      This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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 compound is unstable in solutions, freshly prepared is recommended.

    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: 98.64%

    References
    Cell Assay
    [1]

    Proliferating cells are treated with or without NSC 74859 (30-100 μM) for up to 48 h. In some cases, cells are first transfected with Stat3C, ST3-NT, or ST3-SH2 domain or mock-transfected for 24 h before treatment with compound for an additional 24-48 h. Cells are then detached and analyzed by annexin V binding and flow cytometry to quantify the percent apoptosis[1].

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

    Animal Administration
    [1][3]

    Mice[1]
    Six-week-old female athymic nude mice are used. Athymic nude mice are injected in the left flank area s.c. with 5×106 human breast cancer MDA-MB-231 cells in 100 μL of PBS. After 5-10 days, tumors with a diameter of 3 mm are established. Animals are given NSC 74859 i.v. at 5 mg/kg every 2 or 3 days for 2 weeks and monitored every 2 or 3 days. Animals are stratified so that the mean tumor sizes in all treatment are nearly identical. Tumor volume is calculated according to the formula V=0.52×a2×b, where a is the smallest superficial diameter and b is the largest superficial diameter.
    Rats[3]
    Four-week-old female Wistar Furth rats are used. GH3 cells (5×105 cells in 100 μL Matrigel) are subcutaneously injected into the left lumbar area. After 7 days, tumors with a volume of approximately 100 mm3 are established. Rats are given NSC 74859 intravenously at 5 mg/kg every 2 or 3 days for 2 weeks. Tumor size is measured by caliper measurements twice a week, and volume is calculated as follows: volume=(length×width2)/2. Three weeks after cell inoculations, animals are euthanized and excised tumors are weighed. Blood samples are collected 1 day before S3I-201 treatment and again on the day of euthanization. Serum GH and prolactin are assessed by RIA or ELISA, respectively.

    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. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7370 mL 13.6851 mL 27.3703 mL 68.4257 mL
    5 mM 0.5474 mL 2.7370 mL 5.4741 mL 13.6851 mL
    10 mM 0.2737 mL 1.3685 mL 2.7370 mL 6.8426 mL
    15 mM 0.1825 mL 0.9123 mL 1.8247 mL 4.5617 mL
    20 mM 0.1369 mL 0.6843 mL 1.3685 mL 3.4213 mL
    25 mM 0.1095 mL 0.5474 mL 1.0948 mL 2.7370 mL
    30 mM 0.0912 mL 0.4562 mL 0.9123 mL 2.2809 mL
    40 mM 0.0684 mL 0.3421 mL 0.6843 mL 1.7106 mL
    50 mM 0.0547 mL 0.2737 mL 0.5474 mL 1.3685 mL
    60 mM 0.0456 mL 0.2281 mL 0.4562 mL 1.1404 mL
    80 mM 0.0342 mL 0.1711 mL 0.3421 mL 0.8553 mL
    100 mM 0.0274 mL 0.1369 mL 0.2737 mL 0.6843 mL
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    • 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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