2. NF-κB Cell Cycle/DNA Damage Apoptosis Immunology/Inflammation Metabolic Enzyme/Protease
  3. IKK Topoisomerase Apoptosis NF-κB Reactive Oxygen Species (ROS) Bcl-2 Family
  4. 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.

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

IKKβ-IN-6

IKKβ-IN-6 Chemical Structure

CAS No. : 3117527-91-7

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IKKβ-IN-6 Related Antibodies

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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

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[1].

IC50 & Target[1]

IKKβ

 

Topoisomerase I

 

In Vitro

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.

IKKβ-IN-6 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HCT-116, A549, HepG2, HT-29, RKO, CT-26, THLE-2
Concentration: /
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: HCT-116
Concentration: 0.5, 1, 2.0 μM
Incubation Time: 24 h
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.
In Vivo

IKKβ-IN-6 (2.5-5 mg/kg; i.p.; once every other day; 12 days) potently inhibits colorectal tumor growth in BALB/c mice[1].

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

Animal Model: BALB/c (female, 5-6 weeks of age, subcutaneous CT-26 cell implantation)[1]
Dosage: 2.5 mg/kg; 5 mg/kg
Administration: i.p.; every other day; 12 days
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.
Molecular Weight

758.77

Formula

C43H38N2O11
CAS No.
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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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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IKKβ-IN-6 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:

IKKβ-IN-63117527-91-7IKKTopoisomeraseApoptosisNF-κBReactive Oxygen Species (ROS)Bcl-2 FamilyIκB kinaseI kappa B kinase Nuclear factor-κBNuclear factor-kappaBTopo IA549colorectal cancerHT-29IKKβHepG2IκBαHCT-116p65Inhibitorinhibitorinhibit

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