2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. STAT Apoptosis Bcl-2 Family
  4. STAT3-IN-13

STAT3-IN-13 (compound 6f) is a potent STAT3 inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to the STAT3 SH2 domain with a KD of 0.46 μM. STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705 and downstream target gene expression. STAT3-IN-13 induces apoptosis in vitro and suppresses the growth and metastasis of tumor in vivo. STAT3-IN-13 can be used for cancer research.

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STAT3-IN-13 Chemical Structure

STAT3-IN-13 Chemical Structure

CAS No. : 2248552-86-3

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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1 mg USD 200 In-stock
5 mg USD 400 In-stock
10 mg USD 520 In-stock
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Based on 1 publication(s) in Google Scholar

STAT3-IN-13 Related Antibodies

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Description

STAT3-IN-13 (compound 6f) is a potent STAT3 inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to the STAT3 SH2 domain with a KD of 0.46 μM. STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705 and downstream target gene expression. STAT3-IN-13 induces apoptosis in vitro and suppresses the growth and metastasis of tumor in vivo. STAT3-IN-13 can be used for cancer research[1].

In Vitro

STAT3-IN-13 (compound 6f) (48 hours) has anti-proliferative activity with IC50 values of 0.25, 0.11 and 0.55 μM for 143B, HOS and MG63 cells, respectively[1].
STAT3-IN-13 (compound 6f) (0.001-100 μM) binds to STAT3 and interacts with STAT3586−685 in a concentration dependent manner with a KD of 0.96 μM[1].
STAT3-IN-13 (compound 6f) (0-1.0 μM; 24 hours; 143B and HOS cells) inhibits STAT3 Y705 phosphorylation and suppresses STAT3 in tumor cells[1].
STAT3-IN-13 (compound 6f) (0-1.0 μM; 48 hours; 143B cells) induces apoptosis in a dose-dependent manner[1].

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

STAT3-IN-13 Related Antibodies

Apoptosis Analysis[1]

Cell Line: 143B cells
Concentration: 0, 0.2, 0.5, and 1 μM
Incubation Time: 48 hours
Result: Increased the percentage of apoptosis rates of 3.4%, 8.7%, 10.7%, and 23.3% at 0, 0.2, 0.5 and 1 μM, respectively.

Western Blot Analysis[1]

Cell Line: 143B and HOS cells
Concentration: 0, 0.2, 0.5 and 1.0 μM
Incubation Time: 24 hours
Result: Inhibited STAT3 Y705 phosphorylation and downstream target gene expression including Bcl-2 and VEGF, retained good antitumor activities against control tumor cells without STAT3 knockdown.
In Vivo

STAT3-IN-13 (compound 6f) (10-20 mg/kg; i.p.; twice daily, for 4 weeks; nude mice) blocks osteosarcoma growth and metastasis in vivo[1].

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

Animal Model: Nude mice
Dosage: 10 and 20 mg/kg
Administration: Intraperitoneal injection; twice daily, for 4 weeks
Result: Suppressed tumor weight at a dose of 10 mg/kg.
Molecular Weight

436.49

Formula

C21H20N6O3S
CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

N#CC1=C(SC2=C1CCN(C2)C(NC3=CC=C(C=C3)OC)=O)NC(C(C=N4)=CN4C)=O
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 : 125 mg/mL (286.38 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 2.2910 mL 11.4550 mL 22.9100 mL
5 mM 0.4582 mL 2.2910 mL 4.5820 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.

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  • Dilution Calculator

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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 (14.32 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 6.25 mg/mL.

    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.
  • Protocol 2

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

    Solubility: 6.25 mg/mL (14.32 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 6.25 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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
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 2.2910 mL 11.4550 mL 22.9100 mL 57.2751 mL
5 mM 0.4582 mL 2.2910 mL 4.5820 mL 11.4550 mL
10 mM 0.2291 mL 1.1455 mL 2.2910 mL 5.7275 mL
15 mM 0.1527 mL 0.7637 mL 1.5273 mL 3.8183 mL
20 mM 0.1146 mL 0.5728 mL 1.1455 mL 2.8638 mL
25 mM 0.0916 mL 0.4582 mL 0.9164 mL 2.2910 mL
30 mM 0.0764 mL 0.3818 mL 0.7637 mL 1.9092 mL
40 mM 0.0573 mL 0.2864 mL 0.5728 mL 1.4319 mL
50 mM 0.0458 mL 0.2291 mL 0.4582 mL 1.1455 mL
60 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9546 mL
80 mM 0.0286 mL 0.1432 mL 0.2864 mL 0.7159 mL
100 mM 0.0229 mL 0.1146 mL 0.2291 mL 0.5728 mL
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STAT3-IN-13 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.

Keywords:

STAT3-IN-132248552-86-3STATApoptosisBcl-2 FamilySTAT3apoptosisBcl-2VEGFphosphorylationSTAT3 SH2143B cellsInhibitorinhibitorinhibit

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