1. NF-κB Apoptosis
  2. NF-κB Apoptosis
  3. NF-κB-IN-16

NF-κB-IN-16 (compound 9) 是 NF-κB 抑制剂与 Cisplatin (HY-17394) 的复合物 (Pt(IV) 复合物),具有高效低毒的抗肿瘤活性。NF-κB-IN-16 可引起 DNA 损伤,诱导线粒体功能障碍,产生活性氧,并通过线粒体途径和内质网应激诱导细胞凋亡 (apoptosis)。NF-κB-IN-16 有效抑制 NF-κB/MAPK 信号通路并破坏 PI3K/AKT 信号转导。NF-κB-IN-16 还在 A549 或 A549/CDDP 异种移植模型中优异的体内抗肿瘤效率和低毒性。

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NF-κB-IN-16 Chemical Structure

NF-κB-IN-16 Chemical Structure

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查看 NF-κB 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

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.

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.
体内研究
(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: 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.
分子量

837.01

Formula

C26H35Cl3N2O10Pt

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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产品名称:
NF-κB-IN-16
目录号:
HY-158156
需求量: