STAT3-IN-3
Based on 8 publication(s) in Google Scholar
STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research.
For research use only. We do not sell to patients.
- Purity : 98.40%
- CAS No.: 2361304-26-7
- Formula: C27H26BrN3O6S
- Molecular Weight:600.48
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) STAT3-IN-3
More- Cell Rep Med. 2024 Mar 19;5(3):101472. [Abstract]
- Phytomedicine. 2024 Dec:135:156022. [Abstract]
- Int Immunopharmacol. 2026 Oct 1:186:117075.
- Sci Rep. 2024 Sep 5;14(1):20794. [Abstract]
- J Cell Mol Med. 2026 Feb;30(3):e71050. [Abstract]
- Biochem Biophys Res Commun. 2021 Mar 5:543:29-37. [Abstract]
- Research Square Preprint. 2021 Sep.
- Research Square Preprint. 2021 Apr.
Biological Activity
Description
IC50 & Target
[1]|
STAT3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
1.89 μM
Compound: 7a
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Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 31048139] |
| HepG2 | IC50 |
2.88 μM
Compound: 7a
|
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 31048139] |
| L02 | IC50 |
35.6 μM
Compound: 7a
|
Cytotoxicity against human LO2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human LO2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 31048139] |
| MCF-10A | IC50 |
14.62 μM
Compound: 7a
|
Cytotoxicity against human MCF10A cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human MCF10A cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 31048139] |
| MCF7 | IC50 |
3.33 μM
Compound: 7a
|
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 31048139] |
| MDA-MB-231 | IC50 |
1.43 μM
Compound: 7a
|
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 31048139] |
In Vitro
STAT3-IN-3 has no influence on the phosphorylation levels of STAT1, JAK2, Src and Erk1/2[1].
?
STAT3-IN-3 inhibits the growth of MDA-MB-231, HCT-116, HepG2, and MCF-7 cells with IC50s of 1.43 μM, 1.89 μM, 2.88 μM, and 3.33 μM, respectively[1].
?
STAT3-IN-3 down-regulates the expression of STAT3 target genes Bcl-2 and Cyclin D1[1].
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STAT3-IN-3 inhibits STAT3 tyrosine phosphorylation and serine phosphorylation[1].
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STAT3-IN-3 inhibits STAT3 DNA-binding activity[1].
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STAT3-IN-3 (1-4 μM; 24 hours) increases ROS production and remarkably reduces the mitochondrial membrane potential to induce mitochondrial apoptotic pathway[1].
?
STAT3-IN-3 (1-4 μM; 24 hours) can induce the cleavage of caspase-9, caspase-3 and PARP[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, HCT-116 cells, HepG2 cells, MCF-7cells
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Concentration:MTT assay
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Incubation Time:48 hours
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Result:Exhibited anti-proliferative activity.
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Cell Line:MDA-MB-231 cells
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Concentration:0 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:24 hours
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Result:Induced the apoptosis of MDA-MB-231 cells dose-dependently and the apoptosis rates.
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Cell Line:MDA-MB-231 cells
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Concentration:0 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:24 hours
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Result:Induced the cleavage of caspase-9, caspase-3 and PARP.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult female BALB/c mice (6 weeks of age)[1]
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Dosage:10 mg/kg, 20 mg/kg
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Administration:Intraperitoneal injection, daily, for 14 days
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Result:Significantly inhibited tumor volume.
Chemical Information
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CAS No. 2361304-26-7
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Appearance Solid
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Molecular Weight 600.48
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Formula C27H26BrN3O6S
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Color Light yellow to yellow
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SMILES
BrC1=C2C(S(C(C(N3CCN(C(C4=CC5=CC=C(N(CC)CC)C=C5OC4=O)=O)CC3)=O)=C2)(=O)=O)=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
STAT3 couples activated tyrosine kinase signaling to the oncogenic core transcriptional regulatory circuitry of anaplastic large cell lymphoma. [Abstract]2024 Mar 19;5(3):101472. PMID: 38508140 -
Phytomedicine
Hypocrellin A against intrahepatic Cholangiocarcinoma via multi-target inhibition of the PI3K-AKT-mTOR, MAPK, and STAT3 signaling pathways. [Abstract]2024 Dec:135:156022. PMID: 39284270 -
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Sci Rep
Downregulation of CIAPIN1 regulates the proliferation, migration and glycolysis of breast cancer cells via inhibition of STAT3 pathway. [Abstract]2024 Sep 5;14(1):20794. PMID: 39242716 -
J Cell Mol Med
Exosomal HMGB1 Orchestrates NSCLC Progression and Immunosuppressive Macrophage Polarisation Through the TLR4/NF-κB/IL-6/STAT3 Signalling Cascade. [Abstract]2026 Feb;30(3):e71050. PMID: 41645802 -
Biochem Biophys Res Commun
Suppression of PAPP-A mitigates atherosclerosis by mediating macrophage polarization via STAT3 signaling. [Abstract]2021 Mar 5:543:29-37. PMID: 33508770 -
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Solvent & Solubility
In Vitro:
DMSO : 5 mg/mL (8.33 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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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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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (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)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6653 mL | 8.3267 mL | 16.6533 mL | 41.6334 mL |
| 5 mM | 0.3331 mL | 1.6653 mL | 3.3307 mL | 8.3267 mL |