IKKβ-IN-6
IKKβ-IN-6 is an antitumor agent. IKKβ-IN-6 inhibits IKKβ (IC50: 18.24 μM), thereby suppressing the phosphorylation of p65 and IκBα, blocking the nuclear translocation of p65, and subsequently regulating genes controlled by NF-κB. IKKβ-IN-6 also targets topoisomerase I (Topo I), induces DNA damage, ROS accumulation, loss of mitochondrial membrane potential, and S-phase arrest. IKKβ-IN-6 is applicable to related research on colorectal cancer.
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- CAS No.: 3117527-91-7
- Formule: C43H38N2O11
- Masse moléculaire:758.77
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
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IKKβ |
Topoisomerase I |
IKKβ-IN-6 (compound 6i1) (0.84-8.25 μM; 24 h) exhibits in vitro cytotoxicity against various cancer cell lines[1].
IKKβ-IN-6 (2.0 μM; 24 h) significantly inhibits topoisomerase I (Topo I) activity in HCT-116 cells, with an inhibition rate of 96.37%[1].
IKKβ-IN-6 (0.5-2.0 μM; 24 h) reduces Topo I protein levels, upregulates γH2AX expression, inhibits the NF-κB pathway, and regulates apoptosis-related proteins in HCT-116 cells in a dose-dependent manner[1].
IKKβ-IN-6 (0.5-2.0 μM; 24 h) induces apoptosis in HCT-116 cells in a dose-dependent manner, with the proportions of apoptotic cells reaching 52.55%, 65.06% and 79.20% at concentrations of 0.5 μM, 1.0 μM and 2.0 μM, respectively[1].
IKKβ-IN-6 (0.5-2.0 μM; 24 h) concentration-dependently induces S-phase arrest, elevates intracellular ROS levels, reduces mitochondrial membrane potential, and inhibits cell migration and invasion in HCT-116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116, A549, HepG2, HT-29, RKO, CT-26, THLE-2
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Concentration:/
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Incubation Time:24 h
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Result:Exhibited an IC50 of 0.84 μM against HCT-116 cells.
Exhibited an IC50 of 5.36 μM against A549 cells.
Exhibited an IC50 of 8.25 μM against HepG2 cells.
Exhibited an IC50 of 1.45 μM against HT-29 cells.
Exhibited an IC50 of 5.19 μM against RKO cells.
Exhibited an IC50 of 1.29 μM against CT-26 cells.
Showed an IC50 of >16 μM against THLE-2 cells.
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Cell Line:HCT-116
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Concentration:0.5, 1, 2.0 μM
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Incubation Time:24 h
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Result:Dose-dependently reduced Topo I protein levels and increased γH2AX expression.
Dose-dependently decreased phosphorylation of p65 and IκBα, reduced nuclear p65 levels, and increased cytoplasmic p65 levels.
Upregulated pro-apoptotic Bax protein levels and downregulated anti-apoptotic Bcl-2, Bcl-xl, and Mcl-1 protein levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 5-6 weeks of age, subcutaneous CT-26 cell implantation)[1]
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Dosage:2.5 mg/kg; 5 mg/kg
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Administration:i.p.; every other day; 12 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 64.88% at 2.5 mg/kg.
Achieved a TGI rate of 89.91% at 5 mg/kg.
Caused no significant body weight loss, indicating low toxicity.
Chemical Information
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CAS No. 3117527-91-7
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Masse moléculaire 758.77
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Formule C43H38N2O11
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SMILES
O=C(C([C@@H]1CC/C(COC(C2=CC=CC=C2C(OC3=CC4=CC5=C(N=C4C=C3)C6=CC7=C(C(N6C5)=O)COC([C@]7(O)CC)=O)=O)=O)=C\CC8)=C)O[C@@H]1[C@H]9O[C@@]98C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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