STAT3/NF-κB-IN-1
STAT3/NF-κB-IN-1 is a potentSTAT3 and NF-κB inhibitor with IC50s of 5.86 (STAT3) and 4.22 μM (NF-κB) in 4T1 cells. STAT3/NF-κB-IN-1 is able to induce apoptosis via its upregulation on key apoptotic regulators; caspases-3/9, Bax and downregulation of Bcl-2. STAT3/NF-κB-IN-1 exerts considerable anticancer activity against breast cancer cell lines and reduces tumor volume in vivo. STAT3/NF-κB-IN-1 can be used for the study of breast cancer.
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- Formel: C27H26N8O3S
- Molecular Weight:542.61
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
NF-κB 4.22 μM (IC50) |
STAT3 5.86 μM (IC50) |
Caspase-3 |
Caspase-9 |
Bcl-2 |
Bax |
In Vitro
STAT3/NF-κB-IN-1 (Compound 12a) (72 h) exhibits cytotoxicity against 4T1, MDA-MB-231, MDA-MB-468 and MCF-7 cells with IC50s of 7.68, 1.53, 7.00 and 6.14 μM, respectively[1].
STAT3/NF-κB-IN-1 (10 μM, 24 h) significantly inhibits cell migration and invasion in 4T1 and MDA-MB-231 cells[1].
STAT3/NF-κB-IN-1 (1-10 μM, 24-72 h) significantly induces early MDA-MB-231 cell apoptosis with increasement activity of caspase 3/9 and increasement of Bax/Bcl-2[1].
STAT3/NF-κB-IN-1 (1-5 μM, 48-96 h) significantly inhibits the expressions of p-STAT3 and NF-κB[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:4T1 and MDA-MB-231 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Showed the percentage of scratch closure corresponding to cell migration of 15%.
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Cell Line:MDA-MB-231
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Concentration:1, 2.8, 6 and 10 μM
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Incubation Time:24, 48 and 72 h
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Result:Considerably raised the percentage of apoptotic cells positive to annexin V FITC.
Increased early (ranging from 0.55 % to 22.51 %) and late apoptosis (ranging from 0.18 % to 16.07 %).
Had dose-dependent (1, 2.8 and 6 μM for 48 h) and time dependent (2.8 μM for 24, 48 and 72 h) effects on caspase-9 expression.
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Cell Line:MDA-MB-231 cells
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Concentration:1, 1.5, 2 and 5 μM
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Incubation Time:48, 72 and 96 h
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Result:Inhibited the phosphorylation of p-STAT3 Y705 protein as well as slightly downregulate the expression level of total STAT3.
Clearly suppressed NF-κB protein levels.
Had dose-dependent (1, 2 and 5 μM for 72 h) and time-dependent effects (2 μM for 48, 72 and 96 h) p-SAT3 and NF-κB 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:Ehrlich solid carcinoma model established in BALB/c mice[1]
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Dosage:40 mg/kg
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Administration:Subcutaneous injection (s.c.), once daily for 12 days
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Result:Decreased the tumor volume by 70-80%, and there was no significant toxicity.
Chemical Information
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Molecular Weight 542.61
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Formel C27H26N8O3S
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SMILES
CCN1C(SCC(N/N=C\C2=CN(N=C2C3=CC=CC=C3)C4=CC=CC=C4)=O)=NC5=C1C(N(C(N5C)=O)C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
STAT3/NF-κB-IN-1 Related Classifications
HY-175227 Related Classifications
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