1. Metabolic Enzyme/Protease JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  2. Oxidative Phosphorylation STAT Ferroptosis
  3. W1131

W1131 is a potent STAT3 inhibitor, triggering ferroptosis. W1131 suppresses cancer progression in gastric cancer cell subcutaneous xenograft model, organoids model, and PDX model. W1131 effectively alleviates chemical resistance of cancer cells to 5-FU (HY-90006). W1131 regulates cell cycle, DNA damage response, and oxidative phosphorylation, including IL6-JAK-STAT3 pathway and ferroptosis pathway.

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W1131 Chemical Structure

W1131 Chemical Structure

CAS No. : 2740522-79-4

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5 mg USD 300 In-stock
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25 mg USD 960 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

W1131 is a potent STAT3 inhibitor, triggering ferroptosis. W1131 suppresses cancer progression in gastric cancer cell subcutaneous xenograft model, organoids model, and PDX model. W1131 effectively alleviates chemical resistance of cancer cells to 5-FU (HY-90006). W1131 regulates cell cycle, DNA damage response, and oxidative phosphorylation, including IL6-JAK-STAT3 pathway and ferroptosis pathway[1].

Cellular Effect
Cell Line Type Value Description References
AGS IC50
1.28 μM
Compound: 8; W1131
Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36283181]
MGC-803 IC50
0.79 μM
Compound: 8; W1131
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36283181]
In Vitro

W1131 (0-2 μM; 72 h) inhibits cell survival, migration, and invasion in gastric cancer AGS cell, and also inhibits colony formation for 3 days treatment[1].
W1131 (0.1-3 μM; 24 h) potently inhibits the phosphorylation of STAT3 in AGS cells[1].
W1131 (1 μM; 48 h) triggers ferroptosis and suppresses GPX4, SLC7A11, and FTH1 expression in gastric cancer[1].

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

Western Blot Analysis[1]

Cell Line: AGS cells
Concentration: 0.1 μM, 0.3 μM, 1 μM, and 3 μM
Incubation Time: 24 hours
Result: Dose-dependently decreased the phosphorylated Y705-STAT3, but not STAT5, JAK2, and AKT.

Immunofluorescence[1]

Cell Line: AGS cells
Concentration: 0.3 μM, 1 μM
Incubation Time: 12 hours
Result: Significantly promoted lipid ROS formation, and induced Fe2+ accumulation.
In Vivo

W1131 (3 mg/kg, 10 mg/kg; i.p.; once daily for 2 weeks) inhibits tumor growth dose-dependently, and induces ferroptosis in MGC803 subcutaneous xenograft model in BALB/c-nu/nu mice[1].

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

Animal Model: MGC803 subcutaneous xenografts in mouse[1]
Dosage: 3 mg/kg, 10 mg/kg
Administration: Intraperitoneal injection; once daily for 2 weeks
Result: Inhibited GPX4, SLC7A11, and FTH1 expression level, indicating the induction of ferroptosis.
Caused insignificant change of body weight.
Molecular Weight

429.43

Formula

C23H19N5O4

CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C(C1=CC=C([N+]([O-])=O)O1)NC2=CC=C(C3=CN=C4C=C(C5=CCNCC5)C=CN43)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (232.87 mM; ultrasonic and warming and heat to 160°C; 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 2.3287 mL 11.6433 mL 23.2867 mL
5 mM 0.4657 mL 2.3287 mL 4.6573 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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

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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: 2.5 mg/mL (5.82 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (5.82 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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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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 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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3287 mL 11.6433 mL 23.2867 mL 58.2167 mL
5 mM 0.4657 mL 2.3287 mL 4.6573 mL 11.6433 mL
10 mM 0.2329 mL 1.1643 mL 2.3287 mL 5.8217 mL
15 mM 0.1552 mL 0.7762 mL 1.5524 mL 3.8811 mL
20 mM 0.1164 mL 0.5822 mL 1.1643 mL 2.9108 mL
25 mM 0.0931 mL 0.4657 mL 0.9315 mL 2.3287 mL
30 mM 0.0776 mL 0.3881 mL 0.7762 mL 1.9406 mL
40 mM 0.0582 mL 0.2911 mL 0.5822 mL 1.4554 mL
50 mM 0.0466 mL 0.2329 mL 0.4657 mL 1.1643 mL
60 mM 0.0388 mL 0.1941 mL 0.3881 mL 0.9703 mL
80 mM 0.0291 mL 0.1455 mL 0.2911 mL 0.7277 mL
100 mM 0.0233 mL 0.1164 mL 0.2329 mL 0.5822 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.

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W1131
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