1. NF-κB Apoptosis
  2. NF-κB Apoptosis
  3. 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.

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NF-κB-IN-16 Chemical Structure

NF-κB-IN-16 Chemical Structure

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Description

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[1].

In Vitro

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.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 5 μM
Incubation Time: 24 h
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.

Immunofluorescence[1]

Cell Line: A549 cells
Concentration: 5 μM
Incubation Time: 24 h
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.
In Vivo

NF-κB-IN-16 (compound 9) (5, 13.9 mg/kg; ip; 21 d) showed excellent anti-tumor efficacy in the A549 xenograft nude mouse model, with an inhibition rate of 36.2 at two doses. % and 63.7%[1].
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.

Animal Model: A549 xenograft nude mice models[1]
Dosage: 13.9 mg/kg, equal to the molar amount of cisplatin (5 mg/kg)
Administration: IP; once daily for 21 days
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.
Molecular Weight

837.01

Formula

C26H35Cl3N2O10Pt

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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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.

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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.

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Product Name:
NF-κB-IN-16
Cat. No.:
HY-158156
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