2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. STAT Apoptosis
  4. STAT3-IN-11

STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers.

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STAT3-IN-11 Chemical Structure

STAT3-IN-11 Chemical Structure

CAS No. : 2503096-50-0

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Based on 1 publication(s) in Google Scholar

STAT3-IN-11 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE STAT3-IN-11

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STAT3 STAT5 STAT6 STAT1

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Description

STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers[1].

IC50 & Target

IC50: 1.93 μM (SIP), ≥ 30 μM (SphK1), ≈ 30 μM (SphK2)[1].
In Vitro

STAT3-IN-11 (20 μM, 48 h) has 97.86% inhibitory effect on MDA-MB-231 cells[1].
STAT3-IN-11 (0-30 μM, 48 h) inhibits several cancer cells with IC50 values of 6.01 μM (MDA-MB-231), 7.02μM (HepG2, A549), and normal human cells with IC50 values of 26.54 μM (MDA-MB-10A), 26.69 μM (PBMCs), 12.52 μM (HFL-1) [1].
STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the phosphorylation of STAT3 (stimulated by IL-6 in MDA-MB-231) at site pTyr705 in a dose-dependent manner[1].
STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the expression of the downstream gene (Survivin and Mcl-1) of STAT3 in a concentration-dependent manner[1].
STAT3-IN-11 (2.5-10 μM, 6 h) has no effects on the typical upstream kinases of STAT3 such as p-JAK2 and p-Src and the phosphorylation of STAT1 (a STAT isoform) [1].
STAT3-IN-11 (2.5-10 μM, 48 h) can induce cell apoptosis in a dose-manner[1].

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

STAT3-IN-11 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 20 μM
Incubation Time: 48 hours
Result: The antiproliferative activity reached 97.86%.

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB231, A549, MDA-MB-10A, PBMCs and HFL-1 cells
Concentration: 20 μM
Incubation Time: 48 hours
Result: Inhibited with IC50 values of 6.01, 7.20, 7.02, 26.54, 25.69 and 12.52 μM for MDA-MB231, A549, MDA-MB-10A, PBMCs and HFL-1 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5,5 and 10 μM
Incubation Time: 6 hours
Result: Decrease the level of p-STAT3 at site pTyr705 in a concentration dependent manner.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5,5 and 10 μM
Incubation Time: 6 hours
Result: Down-regulated the level of STAT3 downstream genes.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 5, 10 and 15 μM
Incubation Time: 48 hours
Result: The percentage of apoptotic cells was 24.4% at a concentration of 15 μM.
Molecular Weight

335.35

Formula

C20H17NO4
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C(NCCC(C1=O)=C(C)C(C2=C1C(O)=CC=C2)=O)C3=CC=CC=C3
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 (298.20 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 2.9820 mL 14.9098 mL 29.8196 mL
5 mM 0.5964 mL 2.9820 mL 5.9639 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

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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    90% Corn Oil

    Solubility: 2.5 mg/mL (7.45 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 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 (25.0 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 2.9820 mL 14.9098 mL 29.8196 mL 74.5490 mL
5 mM 0.5964 mL 2.9820 mL 5.9639 mL 14.9098 mL
10 mM 0.2982 mL 1.4910 mL 2.9820 mL 7.4549 mL
15 mM 0.1988 mL 0.9940 mL 1.9880 mL 4.9699 mL
20 mM 0.1491 mL 0.7455 mL 1.4910 mL 3.7274 mL
25 mM 0.1193 mL 0.5964 mL 1.1928 mL 2.9820 mL
30 mM 0.0994 mL 0.4970 mL 0.9940 mL 2.4850 mL
40 mM 0.0745 mL 0.3727 mL 0.7455 mL 1.8637 mL
50 mM 0.0596 mL 0.2982 mL 0.5964 mL 1.4910 mL
60 mM 0.0497 mL 0.2485 mL 0.4970 mL 1.2425 mL
80 mM 0.0373 mL 0.1864 mL 0.3727 mL 0.9319 mL
100 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7455 mL
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STAT3-IN-11 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-112503096-50-0STATApoptosisSTAT3phosphorylationapoptosisanticancerInhibitorinhibitorinhibit

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