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NF-κB-IN-16

🥰Excellent
Catalog No. T209749

NF-κB-IN-16 (compound 9) is a complex of an NF-κB inhibitor and Cisplatin (Pt(IV) complex) with potent and low-toxicity antitumor activity. It can cause DNA damage, induce mitochondrial dysfunction, generate reactive oxygen species, and trigger apoptosis via mitochondrial pathways and endoplasmic reticulum stress. NF-κB-IN-16 effectively inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signal transduction. Additionally, it demonstrates excellent in vivo antitumor efficacy and low toxicity in A549 or A549/CDDP xenograft models.

NF-κB-IN-16

NF-κB-IN-16

🥰Excellent
Catalog No. T209749
NF-κB-IN-16 (compound 9) is a complex of an NF-κB inhibitor and Cisplatin (Pt(IV) complex) with potent and low-toxicity antitumor activity. It can cause DNA damage, induce mitochondrial dysfunction, generate reactive oxygen species, and trigger apoptosis via mitochondrial pathways and endoplasmic reticulum stress. NF-κB-IN-16 effectively inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signal transduction. Additionally, it demonstrates excellent in vivo antitumor efficacy and low toxicity in A549 or A549/CDDP xenograft models.
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Bioactivity
Description
NF-κB-IN-16 (compound 9) is a complex of an NF-κB inhibitor and Cisplatin (Pt(IV) complex) with potent and low-toxicity antitumor activity. It can cause DNA damage, induce mitochondrial dysfunction, generate reactive oxygen species, and trigger apoptosis via mitochondrial pathways and endoplasmic reticulum stress. NF-κB-IN-16 effectively inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signal transduction. Additionally, it demonstrates excellent in vivo antitumor efficacy and low toxicity in A549 or A549/CDDP xenograft models.
In vitro
NF-κB-IN-16 (compound 9) (5 μM; 24 h) induces apoptosis in A549 cells and arrests the cell cycle in the S phase. It demonstrates cytotoxicity against human cancer cell lines with IC50 values of 0.45 μM (HepG-2), 0.46 μM (HCT-116), 0.73 μM (MCF-7), and 0.29 μM (A549). Additionally, NF-κB-IN-16 (5 μM; 24 h) can induce DNA damage in A549 cells.
In vivo
NF-κB-IN-16 (compound 9), administered intraperitoneally at doses of 5 mg/kg and 13.9 mg/kg for 21 days, demonstrated outstanding antitumor efficacy in an A549 xenograft nude mouse model, with inhibition rates of 36.2% and 63.7%, respectively. Additionally, NF-κB-IN-16 showed significant inhibitory effects in an A549/CDPP xenograft nude mouse model.
Chemical Properties
FormulaC26H35Cl3N2O10Pt
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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