STAT3-IN-10
STAT3-IN-10 is a STAT3 inhibitor with an IC50 value of 5.18 µM. STAT3-IN-10 directly binds to STAT3 SH2 domain, induces cancer cells apoptosis.
For research use only. We do not sell to patients.
- CAS No.: 2499491-04-0
- Formula: C17H13NO5
- Molecular Weight:311.29
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
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STAT3 5.18 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
1.24 μM
Compound: A11
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Antiproliferative activity against human HepG2 cells overexpressed STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against human HepG2 cells overexpressed STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
|
[PMID: 32603980] |
| MDA-MB-231 | IC50 |
0.67 μM
Compound: A11
|
Antiproliferative activity against human MDA-MB-231 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against human MDA-MB-231 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
|
[PMID: 32603980] |
| MDA-MB-468 | IC50 |
0.77 μM
Compound: A11
|
Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
|
[PMID: 32603980] |
In Vitro
STAT3-IN-10 (A11) (48 h) shows IC50 values of 0.67, 0.77, 1.24 µM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively[1].
STAT3-IN-10 (A11) directly binds to the STAT3 SH2 domain [1].
STAT3-IN-10 (A11) (0-3 μM, 24 h) inhibits the phosphorylation of STAT3 and its downstream target proteins and has a good selectivity against the tumor suppressor STAT1 [1].
STAT3-IN-10 (A11) (0-4 μM, 24 h) induces apoptosis in cancer cells[1].
STAT3-IN-10 (A11) (0-4 μM, 24 h) dose-dependently causes a significant S phase arrest in MDA-MB-231 cells[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:Breast cancer cell lines: MDA-MB-231 and MDA-MB-468; human liver carcinoma cell line: HepG2.
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Concentration:
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Incubation Time:48 h, re-incubated for 4 h (MDA-MB-468, MDA-MB-231) and 1h (HepG2).
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Result:Showed IC50 values of 0.67, 0.77, 1.24 µM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively.
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Cell Line:MDA-MB-231.
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Concentration:0, 0.75, 1.5 and 3.0 μM.
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Incubation Time:24 h.
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Result:Decreased the STAT3-Y705 phosphorylation without affecting the total amount of STAT3 protein and decreased the expression of STAT3 target genes, including C-Myc and Cyclin D1 in a dose-dependent manner. Had little impact on the level of STAT1 and its phosphorylation on Tyr701.
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Cell Line:MDA-MB-231.
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Concentration:0, 1, 2, and 4 μM.
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Incubation Time:24 h.
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Result:Induced the apoptosis in MDA-MB-231 cells in a concentration-dependent manner
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Cell Line:MDA-MB-231.
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Concentration:0, 1, 2, and 4 μM.
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Incubation Time:24 h.
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Result:Could dose-dependently cause a significant S phase arrest in MDA-MB-231 cells
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Five weeks old female BALB/c nude mice (16–18g) bearing inoculation of human breast cancer cells MDA-MB-231[1].
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Dosage:5 and 10 mg/kg
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Administration:IP, once a day, 21 days
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Result:Inhibited the growth of human xenograft tumor in vivo without apparent body-weight loss for treated mice and inhibited the levels of p-STAT3 in tumor tissues.
Chemical Information
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CAS No. 2499491-04-0
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Molecular Weight 311.29
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Formula C17H13NO5
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SMILES
COC(C=C1)=CC=C1NC2=CC(C3=C(C2=O)OC(C(C)=O)=C3)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Detection of 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
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)