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

NSC 74859 (Synonyms: S3I-201)

Cat. No.: HY-15146 Purity: 99.50%
Handling Instructions

NSC 74859 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 20 publication(s) in Google Scholar

Top Publications Citing Use of Products

    NSC 74859 purchased from MCE. Usage Cited in: Mol Immunol. 2017 Nov;91:134-144.

    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.

    NSC 74859 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Aug 30.

    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 MCE. Usage Cited in: Cancer Lett. 2018 Aug 28;430:201-214.

    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 MCE. Usage Cited in: Biofactors. 2018 Nov;44(6):570-576.

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

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    NSC 74859 is a selective Stat3 inhibitor with an IC50 of 86 μM.

    IC50 & Target[1]


    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].

    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].

    Molecular Weight




    CAS No.





    Room temperature in continental US; may vary elsewhere.

    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)

    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
    10 mM 0.2737 mL 1.3685 mL 2.7370 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: ≥ 7.5 mg/mL (20.53 mM); Clear solution

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    Cell Assay

    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

    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.
    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.


    Purity: 99.50%

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    NSC 74859S3I-201NSC74859NSC-74859STATInhibitorinhibitorinhibit

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