IKKβ-IN-7
IKKβ-IN-7 is an IKKβ inhibitor with an IC50 value of 9.44 μM. IKKβ-IN-7 induces DNA damage, S-phase cell cycle arrest, ROS accumulation, mitochondrial membrane potential loss, and apoptosis. IKKβ-IN-7 inhibits phosphorylation of p65 and IκBα, suppresses p65 nuclear translocation, and regulates NF-κB-controlled genes. IKKβ-IN-7 suppresses tumor growth in xenograft models and shows activity against colorectal cancer with low normal cell cytotoxicity. IKKβ-IN-7 can be used for the research of colorectal cancer.
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- CAS No.: 3117527-92-8
- Formule: C45H42N2O11
- Masse moléculaire:786.82
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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IKKβ 9.44 μM (IC50) |
p65 |
Bax |
Bcl-2 |
Bcl-xL |
IKKβ-IN-7 (6i2) (24 h) potently inhibits the proliferation of multiple cancer cell lines, including A549 cells (IC50 = 5.11 μM), HepG2 cells (IC50 = 9.81 μM), HCT-116 cells (IC50 = 1.08 μM), HT-29 cells (IC50 = 4.17 μM), RKO cells (IC50 = 4.72 μM), and CT-26 cells (IC50 = 0.86 μM), while showing low cytotoxicity toward normal transformed human liver epithelial THLE-2 cells (IC50 > 16 μM)[1].
IKKβ-IN-7 (1 h) directly inhibits IKKβ kinase activity with an IC50 of 9.44 μM[1].
IKKβ-IN-7 (2.0 μM; 30 min) potently inhibits Topo I activity, achieving a 96.84% inhibition rate at a concentration of 2.0 μM after 30 min incubation at 37°C[1].
IKKβ-IN-7 (0.5-2.0 μM; 24 h) exerts multiple biological effects on HCT-116 cells in vitro in a dose-dependent manner: induces DNA damage via increased γ-H2AX expression and reduces Topo I protein levels (maximal effects at 2.0 μM); dose-dependently inhibits the phosphorylation of IκBα and p65 to suppress NF-κB pathway activation; inhibits p65 nuclear translocation without altering total p65 protein levels; modulates Bcl-2 family protein expression (increases pro-apoptotic Bax and decreases anti-apoptotic Bcl-2, Bcl-xl, and Mcl-1) indicating induction of mitochondria-mediated apoptosis; induces apoptosis with a 68.29% apoptosis rate at 2.0 μM; induces S-phase cell cycle arrest with 44.6% of cells in S phase at 2.0 μM; increases intracellular ROS levels; reduces mitochondrial membrane potential[1].
IKKβ-IN-7 (0.5-2.0 μM; 24 h, 48 h) inhibits wound healing migration of human colorectal carcinoma HCT-116 cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human colorectal carcinoma HCT-116 cells
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Concentration:0.5, 1, 2.0 μM
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Incubation Time:24 h
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Result:Decreased Topo I levels by more than 50% at 2.0 μM, and increased γ-H2AX expression by 2–3-fold in a dose-dependent manner compared with untreated controls.
Reduced the phosphorylation levels of IκBα and p65 gradually to less than 0.5-fold of control levels as concentration increased from 0.5 to 2.0 μM.
Left total p65 protein levels unchanged, but decreased nuclear p65 levels significantly and increased cytoplasmic p65 levels in a dose-dependent manner compared with controls.
Increased Bax expression in a dose-dependent manner, while significantly reduced the expression of anti-apoptotic proteins Bcl-2, Bcl-xL and Mcl-1 in a dose-dependent manner.
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Cell Line:human colorectal carcinoma HCT-116 cells
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Concentration:0.5, 1, 2.0 μM
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Incubation Time:24 h
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Result:Induced apoptosis rates of 39.45% (0.5 μM), 58.14% (1.0 μM), and 68.29% (2.0 μM), compared to 8.86% in untreated controls.
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Cell Line:human colorectal carcinoma HCT-116 cells
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Concentration:0.5, 1, 2.0 μM
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Incubation Time:24 h
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Result:Induced S-phase arrest, with the proportion of cells in S phase reaching 44.6% at 2.0 μM, in a dose-dependent manner.
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Cell Line:human colorectal carcinoma HCT-116 cells
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Concentration:0.5, 1, 2.0 μM
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Incubation Time:24 h; 48 h
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Result:Inhibited wound healing in a dose-dependent manner, with wound healing rates of 25.23% (24 h, 0.5 μM), 5.70% (24 h, 1.0 μM), 4.69% (24 h, 2.0 μM), 69.67% (48 h, 0.5 μM), 54.78% (48 h, 1.0 μM), and 18.35% (48 h, 2.0 μM), compared to 43.05% (24 h) and 94.61% (48 h).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female immunocompetent BALB/c mice (5-6 weeks old) were subcutaneously injected with CT-26 cells (3 × 106 cells per mouse in 100 μL sterile PBS)[1]
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Dosage:2.5 mg/kg, 5 mg/kg
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Administration:Intraperitoneal (IP) injection; once every other day
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Result:Exhibited potent antitumor efficacy with tumor growth inhibition (TGI) rates of 68.81% (2.5 mg/kg) and 95.41% (5 mg/kg).
No significant body weight loss or animal mortality observed during the treatment period.
H&E staining of major organs (heart, liver, spleen, lung, kidney) revealed no obvious morphological abnormalities.
Superior safety profile compared to 10-HCPT (which caused inflammatory cell infiltration in spleen and glomerular atrophy in kidney at 2.5 mg/kg).
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Animal Model:Female immunocompetent BALB/c mice (20.0 g) were used for acute toxicity test[1]
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Dosage:2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg, 60 mg/kg
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Administration:Intraperitoneal (IP) injection; once daily; each dose administered for 2 consecutive days (total 12 days)
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Result:No animal death observed at doses up to 20 mg/kg.
Minimal lethal dose (MLD) and median lethal dose (LD50) were determined based on survival status, with lower toxicity than 10-HCPT (which caused mortality at 5 mg/kg).
Chemical Information
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CAS No. 3117527-92-8
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Masse moléculaire 786.82
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Formule C45H42N2O11
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SMILES
O=C(C([C@@H]1CC/C(COC(C2=CC=CC=C2C(OC3=CC4=C(C5=C(N=C4C=C3)C6=CC7=C(C(N6C5)=O)COC([C@]7(O)CC)=O)CC)=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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