NF-κB-IN-16
NF-κB-IN-16 (compound 9) is a complex (Pt(IV) complex) of NF-κB inhibitor and Cisplatin (HY-17394), which has high efficacy and low toxicity in anti-tumor activity. active. NF-κB-IN-16 can cause DNA damage, induce mitochondrial dysfunction, produce reactive oxygen species, and induce apoptosis through the mitochondrial pathway and endoplasmic reticulum stress. NF-κB-IN-16 potently inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signaling. NF-κB-IN-16 also exhibits excellent in vivo antitumor efficiency and low toxicity in A549 or A549/CDDP xenograft models.
For research use only. We do not sell to patients.
- Formula: C26H35Cl3N2O10Pt
- Molecular Weight:837.01
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
NF-κB-IN-16 (compound 9) (5 μM; 24 h) induces apoptosis in A549 cells, exhibited cell cycle arrest at the S phase[1].
And NF-κB-IN-16 shows cytotoxicity against human cancer cells with IC50s of 0.45 μM (HepG-2), 0.46 μM (HCT-116), 0.73 μM (MCF-7), and 0.29 μM (A549), respectively[1].
NF-κB-IN-16 (5 μM; 24 h) could induce DNA damage in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Showed the strongest cell apoptosis induction rate of 39.43% among cisplatin (5 μM), and the mixture of cisplatin and the Pt(IV) complex group.
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Cell Line:A549 cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Observed long comet tail formation in the cisplatin, cisplatin/4 mixture, and Pt(IV) complex, in comet assay
Caused stronger DNA damage by Pt(IV) complex, than that caused by cisplatin (5 μM) or cotherapy, respectively.
NF-κB-IN-16 also showed significant inhibitory effects on the A549/CDPP xenograft nude mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549 xenograft nude mice models[1]
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Dosage:13.9 mg/kg, equal to the molar amount of cisplatin (5 mg/kg)
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Administration:IP; once daily for 21 days
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Result:Resulted stronger inhibition (72.7%) on tumor growth, than that of CDDP (60.4%) and the combination group (68.5%), respectively
Showed low toxicity side effect against mouse body weight.
Chemical Information
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Molecular Weight 837.01
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Formula C26H35Cl3N2O10Pt
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SMILES
COC1=C(C(OC)=CC(C(/C=C/C2=CC=C(C(OCCOC(CCCC(O[Pt]([NH3])(Cl)(Cl)([NH3])Cl)=O)=O)=C2)OC)=O)=C1)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)