2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. STAT Ferroptosis Apoptosis Glutathione Peroxidase Bcl-2 Family Reactive Oxygen Species (ROS)
  4. 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.

For research use only. We do not sell to patients.

STAT3-IN-51

STAT3-IN-51 Chemical Structure

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STAT3-IN-51 Related Antibodies

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GPX1 GPX4

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Description

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[1].

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.

STAT3-IN-51 Related Antibodies

Apoptosis Analysis[1]

Cell Line: SW480
Concentration: 0.3 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: SW480
Concentration: 0.3 μM
Incubation Time: 24 h
Result: Significantly suppressed both total STAT3 and p-STAT3 expression in SW480 cells, demonstrating dual inhibition of STAT3.
Significantly suppressed GPX4 expression.
In Vivo

STAT3-IN-51 (Compound 8d) (5-10 mg/kg, i.p. every two days for 13 days) significantly inhibits tumor growth in a CT26 tumor xenograft model, with higher efficacy and better safety profile[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c mice (5-week-old) bearing CT26 tumor xenografts[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: i.p. (intraperitoneal); every two days for 13 days
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.
Molecular Weight

651.59

Formula

C36H27F6NO4
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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STAT3-IN-51 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

STAT3-IN-51STATFerroptosisApoptosisGlutathione PeroxidaseBcl-2 FamilyReactive Oxygen Species (ROS)STAT3 inhibitorapoptosisferroptosisimmunogenic cell deathROS generationdecreases Bcl-2 expressiondisruptes mitochondrial functionsuppresses GPX4 activitycolorectal carcinomabreast adenocarcinomanon-small cell lung cancer (NSCLC) and cisplatin-resistant pulmonary adenocarcinomaInhibitorinhibitorinhibit

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