STAT3-IN-51
STAT3-IN-51 is a STAT3 inhibitor that directly binds to the STAT3 SH2 domain. STAT3-IN-51 induces apoptosis, ferroptosis, and immunogenic cell death (ICD) to potentiate anti-tumor immunity. STAT3-IN-51 inhibits STAT3 activation (phosphorylation, p-STAT3) and its downstream signaling. STAT3-IN-51 induces ROS generation, decreases Bcl-2 expression, disruptes mitochondrial function, suppresses GPX4 activity, and promotes lipid peroxidation. STAT3-IN-51 can be used for the study of colorectal carcinoma, breast adenocarcinoma, non-small cell lung cancer (NSCLC) and Cisplatin (HY-17394)-resistant pulmonary adenocarcinoma.
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- 화학식: C36H27F6NO4
- 분자량:651.59
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
STAT3 |
GPX4 |
Bcl-2 |
In Vitro
STAT3-IN-51 (Compound 8d) (48 h) exhibits IC50 values of 0.26 μM, 0.34 μM, 0.61 μM, and 0.67 μM against SW480, MDA-MB-231, A549, and A549/DDP cells, respectively[1].
STAT3-IN-51 (0.3 μM; 24 h) induces apoptosis in SW480 cells through mitochondrial dysfunction and caspase activation[1].
STAT3-IN-51 (0.3 μM; 24 h) effectively inhibits both total STAT3 and p-STAT3 in SW480 cells[1].
STAT3-IN-51 (0.3 μM; 24 h) enhances CD8+ T lymphocyte infiltration and expansion[1].
STAT3-IN-51 (0.3 μM; 24 h) enhances dendritic cell maturation and reduces HMGB1 levels[1].
STAT3-IN-51 (0.3 μM; 24 h) induces ferroptosis in SW480 cells through GPX4 suppression and lipid peroxidation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW480
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Concentration:0.3 μM
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Incubation Time:24 h
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Result:Significantly reduced Bcl-2 expression, increased ROS generation, and induced mitochondrial depolarization. Flow cytometry showed a 8.37% and 30.3% increase in early and late apoptosis in SW480 cells.
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Cell Line:SW480
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Concentration:0.3 μM
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Incubation Time:24 h
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Result:Significantly suppressed both total STAT3 and p-STAT3 expression in SW480 cells, demonstrating dual inhibition of STAT3.
Significantly suppressed GPX4 expression.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice (5-week-old) bearing CT26 tumor xenografts[1]
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Dosage:5 mg/kg, 10 mg/kg
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Administration:i.p. (intraperitoneal); every two days for 13 days
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Result:Achieved 63.17% tumor growth inhibition (TGI) at 5 mg/kg, and 75.62% TGI at 10 mg/kg.
At 10 mg/kg, shows better tolerability.
Had minimal toxicity, with no significant histopathological changes or weight loss.
- Western Blot
- RNA extraction experimental
- Mitochondrial membrane-potential fluorescent assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- Kinase activity and phosphorylation assays
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Apoptosis Solutions
- Ferroptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
Chemical Information
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분자량 651.59
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화학식 C36H27F6NO4
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SMILES
O=C1C(C)=C(CCCC(N2C/C(C(/C(C2)=C/C3=CC=CC(C(F)(F)F)=C3)=O)=C\C4=CC=CC(C(F)(F)F)=C4)=O)C(C5=C1C=CC=C5)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
STAT3-IN-51 Related Classifications
HY-180245 Related Classifications
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Keywords
- STAT3-IN-51
- STAT
- Ferroptosis
- Apoptosis
- Glutathione Peroxidase
- Bcl-2 Family
- Reactive Oxygen Species (ROS)
- STAT3 inhibitor
- apoptosis
- ferroptosis
- immunogenic cell death
- ROS generation
- decreases Bcl-2 expression
- disruptes mitochondrial function
- suppresses GPX4 activity
- colorectal carcinoma
- breast adenocarcinoma
- non-small cell lung cancer (NSCLC) and cisplatin-resistant pulmonary adenocarcinoma
- Inhibitor
- inhibitor
- inhibit