2. NF-κB Cell Cycle/DNA Damage Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation
  3. IKK Topoisomerase Apoptosis NF-κB Reactive Oxygen Species (ROS) Bcl-2 Family
  4. IKKβ-IN-6

IKKβ-IN-6 是一种抗肿瘤剂。IKKβ-IN-6 能够抑制 IKKβ (IC50: 18.24 μM)，进而抑制 p65 和 IκBα 的磷酸化，阻止 p65 的核转位，并随后调控由 NF-κB 控制的基因。IKKβ-IN-6 还可以靶向拓扑异构酶 I (Topo I)，诱导 DNA 损伤、ROS 积累、线粒体膜电位丧失以及 S 期阻滞。IKKβ-IN-6 可用于结直肠癌的相关研究。

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IKKβ-IN-6

IKKβ-IN-6 Chemical Structure

CAS No. : 3117527-91-7

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IKKβ-IN-6 相关抗体

Top Publications Citing Use of Products

查看 IKK 亚型特异性产品:

查看所有亚型
IKK-α IKK-β IKK IKKε TBK1

查看 Topoisomerase 亚型特异性产品:

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Topoisomerase Topo I Topo II DNA gyrase

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IKKβ-IN-6 is an antitumor agent. IKKβ-IN-6 inhibits IKKβ (IC50: 18.24 μM), thereby suppressing the phosphorylation of p65 and IκBα, blocking the nuclear translocation of p65, and subsequently regulating genes controlled by NF-κB. IKKβ-IN-6 also targets topoisomerase I (Topo I), induces DNA damage, ROS accumulation, loss of mitochondrial membrane potential, and S-phase arrest. IKKβ-IN-6 is applicable to related research on colorectal cancer[1].

IC50 & Target[1]

IKKβ

 

Topoisomerase I

 

体外研究
(In Vitro)

IKKβ-IN-6 (compound 6i1) (0.84-8.25 μM; 24 h) 对多种癌细胞系表现出体外细胞毒性[1]。
IKKβ-IN-6 (2.0 μM; 24 h) 在 HCT-116 细胞中显著抑制拓扑异构酶 I（Topo I）活性，抑制率达 96.37%[1]。

IKKβ-IN-6 (0.5-2.0 μM; 24 h) 以剂量依赖方式降低 HCT-116 细胞中 Topo I 蛋白水平，上调 γH2AX 表达，抑制 NF-κB 通路，并调控凋亡相关蛋白[1]。
IKKβ-IN-6 (0.5-2.0 μM; 24 h) 可呈剂量依赖性诱导 HCT-116 细胞发生凋亡，在 0.5 μM、1.0 μM 和 2.0 μM 浓度下的凋亡细胞占比分别为 52.55 %、65.06 % 和 79.20 %[1]。
IKKβ-IN-6 (0.5-2.0 μM; 24 h) 可浓度依赖性地诱导 HCT-116 细胞发生 S 期阻滞和升高细胞内的 ROS 水平，降低线粒体膜电位，并抑制细胞迁移和侵袭[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IKKβ-IN-6 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HCT-116, A549, HepG2, HT-29, RKO, CT-26, THLE-2
Concentration: /
Incubation Time: 24 h
Result: Exhibited an IC50 of 0.84 μM against HCT-116 cells.
Exhibited an IC50 of 5.36 μM against A549 cells.
Exhibited an IC50 of 8.25 μM against HepG2 cells.
Exhibited an IC50 of 1.45 μM against HT-29 cells.
Exhibited an IC50 of 5.19 μM against RKO cells.
Exhibited an IC50 of 1.29 μM against CT-26 cells.
Showed an IC50 of >16 μM against THLE-2 cells.

Western Blot Analysis[1]

Cell Line: HCT-116
Concentration: 0.5, 1, 2.0 μM
Incubation Time: 24 h
Result: Dose-dependently reduced Topo I protein levels and increased γH2AX expression.
Dose-dependently decreased phosphorylation of p65 and IκBα, reduced nuclear p65 levels, and increased cytoplasmic p65 levels.
Upregulated pro-apoptotic Bax protein levels and downregulated anti-apoptotic Bcl-2, Bcl-xl, and Mcl-1 protein levels.
体内研究
(In Vivo)

IKKβ-IN-6 (2.5-5 mg/kg; 腹腔注射; 每隔 1 天 1 次; 12 天) 可强效抑制 BALB/c 小鼠的结直肠肿瘤生长[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (female, 5-6 weeks of age, subcutaneous CT-26 cell implantation)[1]
Dosage: 2.5 mg/kg; 5 mg/kg
Administration: i.p.; every other day; 12 days
Result: Achieved a tumor growth inhibition (TGI) rate of 64.88% at 2.5 mg/kg.
Achieved a TGI rate of 89.91% at 5 mg/kg.
Caused no significant body weight loss, indicating low toxicity.
分子量

758.77

Formula

C43H38N2O11
CAS 号
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

IKKβ-IN-6 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

IKKβ-IN-63117527-91-7IKKTopoisomeraseApoptosisNF-κBReactive Oxygen Species (ROS)Bcl-2 FamilyIκB kinaseI kappa B kinase Nuclear factor-κBNuclear factor-kappaBTopo IA549colorectal cancerHT-29IKKβHepG2IκBαHCT-116p65Inhibitorinhibitorinhibit

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