STAT3-IN-11
Based on 1 publication(s) in Google Scholar
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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- Pureté : 98.29%
- CAS No.: 2503096-50-0
- Formule: C20H17NO4
- Masse moléculaire:335.35
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) STAT3-IN-11
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Activité biologique
Description
IC50 & Target
IC50: 1.93 μM (SIP), ≥ 30 μM (SphK1), ≈ 30 μM (SphK2)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
7.02 μM
Compound: 147
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Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay
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[PMID: 38458106] |
| HepG2 | IC50 |
7.2 μM
Compound: 147
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Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay
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[PMID: 38458106] |
| MDA-MB-231 | IC50 |
6.01 μM
Compound: 147
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Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
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[PMID: 38458106] |
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. Further protocols information, click here.
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Cell Line:MDA-MB-231 cells
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Concentration:20 μM
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Incubation Time:48 hours
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Result:The antiproliferative activity reached 97.86%.
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Cell Line:MDA-MB231, A549, MDA-MB-10A, PBMCs and HFL-1 cells
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Concentration:20 μM
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Incubation Time:48 hours
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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.
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Cell Line:MDA-MB-231 cells
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Concentration:2.5,5 and 10 μM
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Incubation Time:6 hours
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Result:Decrease the level of p-STAT3 at site pTyr705 in a concentration dependent manner.
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Cell Line:MDA-MB-231 cells
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Concentration:2.5,5 and 10 μM
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Incubation Time:6 hours
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Result:Down-regulated the level of STAT3 downstream genes.
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Cell Line:MDA-MB-231 cells
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Concentration:5, 10 and 15 μM
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Incubation Time:48 hours
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Result:The percentage of apoptotic cells was 24.4% at a concentration of 15 μM.
Chemical Information
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CAS No. 2503096-50-0
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Appearance Solid
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Masse moléculaire 335.35
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Formule C20H17NO4
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Color Yellow to orange
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SMILES
O=C(NCCC(C1=O)=C(C)C(C2=C1C(O)=CC=C2)=O)C3=CC=CC=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
STAT3-IN-11 Related Classifications
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