1. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  2. STAT Apoptosis
  3. STAT3-SH2 domain inhibitor 1

STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer.

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STAT3-SH2 domain inhibitor 1 Chemical Structure

STAT3-SH2 domain inhibitor 1 Chemical Structure

CAS No. : 2816059-41-1

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Based on 1 publication(s) in Google Scholar

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Description

STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer[1].

In Vitro

STAT3-SH2 domain inhibitor 1 (compound 7; 1-5 μM; 24 h; AGS and MGC-803 cell lines) strongly and selectively inhibits the STAT3 signaling pathway[1].
STAT3-SH2 domain inhibitor 1 (0-10 μM; 72 h) has antiproliferative activity with IC50 values of 1.54 and 4.73 μM for AGS and MGC-803 cells, respectively[1].
STAT3-SH2 domain inhibitor 1 (1 and 3 μM; 72 h; AGS and MGC-803 cell lines) induces apoptosis effects in gastric cancer cells[1].

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

Cell Viability Assay[1]

Cell Line: AGS and MGC-803 cell lines
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Suppressed cancer cell proliferation and growth.

Apoptosis Analysis[1]

Cell Line: AGS and MGC-803 cell lines
Concentration: 1 and 3 μM
Incubation Time: 72 hours
Result: Induced apoptosis in AGS cells in a concentration-dependent manner, resulting in apoptotic percentages of 13.0 and 26.7% at 1 and 3 μM, respectively.
Induced apoptosis of MGC-803 cells in a dose-dependent way, leading to apoptotic percentage of 11.2% at 5 μM.

Western Blot Analysis[1]

Cell Line: AGS and MGC-803 cell lines
Concentration: 1 and 3 μM
Incubation Time: 24 hours
Result: Inhibited STAT3 phosphorylation at Tyr705 in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: HEK-293T cells
Concentration: 1, 3, and 5 μM
Incubation Time: 24 hours
Result: Disrupted STAT3 dimerization in HEK-293T cells.
In Vivo

STAT3-SH2 domain inhibitor 1 (compound 7; 5 and 15 mg/kg; i.p.; daily, for 20 d) exhibits superior antitumor activity in BALB/c male nude mice with gastric tumor xenografts[1].

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

Animal Model: BALB/c male nude mice with gastric tumor xenografts[1]
Dosage: 5 and 15 mg/kg
Administration: Intraperitoneal injection; daily, for 20 days
Result: Suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) of 65.14% at 5 mg/kg and 79.13% at 15 mg/kg, respectively.
Molecular Weight

610.40

Formula

C28H28BF5N2O5S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C1=CC=C(B(O)O)C=C1)CC2=CC=C(C3CCCCC3)C=C2)CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=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 : 8.33 mg/mL (13.65 mM; ultrasonic and warming and heat to 80°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 1.6383 mL 8.1913 mL 16.3827 mL
5 mM 0.3277 mL 1.6383 mL 3.2765 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: 0.83 mg/mL (1.36 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 0.83 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: 0.83 mg/mL (1.36 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 0.83 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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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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 1.6383 mL 8.1913 mL 16.3827 mL 40.9567 mL
5 mM 0.3277 mL 1.6383 mL 3.2765 mL 8.1913 mL
10 mM 0.1638 mL 0.8191 mL 1.6383 mL 4.0957 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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