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
- 순도&문서
- References
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Help & FAQs
Biological Activity
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STAT3 |
GPX4 |
Bcl-2 |
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.
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.
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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- 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