| Bioactivity | 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.[5][1]. |
| Invitro | NF-κB-IN-16 (compound 9)（5 μM；24 h）诱导 A549 细胞凋亡，将细胞周期停滞在 S 期[1]。 并且 NF-κB-IN-16 对人类表现出细胞毒性，对癌细胞的 IC50 值分别为 0.45 μM (HepG-2)、0.46 μM (HCT-116)、0.73 μM (MCF-7) 和 0.29 μM (A549)[1]。NF-κB-IN-16 (5 μM; 24 h) 可诱导 A549 细胞的 DNA 损伤[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> NF-κB-IN-16 相关抗体: Apoptosis Analysis[1] Cell Line: |
| In Vivo | NF-κB-IN-16 (compound 9) (5, 13.9 mg/kg; ip; 21 d) 在 A549 异种移植裸鼠模型表现出优异的抗肿瘤功效，在两种剂量下的抑制率分别为 36.2% 和 63.7%[1]。NF-κB-IN-16 还对 A549/CDPP 异种移植裸鼠模型表现出显著的抑制作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C26H35Cl3N2O10Pt |
| Molar Mass | 837.01 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Wang M, et al. Novel NF-κB Inhibitor-Conjugated Pt(IV) Prodrug to Enable Cancer Therapy through ROS/ER Stress and Mitochondrial Dysfunction and Overcome Multidrug Resistance. J Med Chem. 2024 Apr 25;67(8):6218-6237. |