2. NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. IKK NF-κB Bcl-2 Family Reactive Oxygen Species (ROS) Apoptosis
  4. IKKβ-IN-7

IKKβ-IN-7 是一种 IKKβ 抑制剂，IC50 值为 9.44 μM。IKKβ-IN-7 可诱导 DNA 损伤、S 期细胞周期阻滞、ROS 积累、线粒体膜电位丢失及凋亡 (apoptosis)。IKKβ-IN-7 可抑制 p65 和 IκBα 的磷酸化，阻断 p65 的核转位，并调控 NF-κB 调控的基因。IKKβ-IN-7 可抑制异种移植模型中的肿瘤生长，对结直肠癌具有活性且对正常细胞的细胞毒性较低。IKKβ-IN-7 可用于结直肠癌的研究。

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IKKβ-IN-7

IKKβ-IN-7 Chemical Structure

CAS No. : 3117527-92-8

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IKKβ-IN-7 相关抗体

Top Publications Citing Use of Products

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IKK-α IKK-β IKK IKKε TBK1

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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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-7 is an IKKβ inhibitor with an IC50 value of 9.44 μM. IKKβ-IN-7 induces DNA damage, S-phase cell cycle arrest, ROS accumulation, mitochondrial membrane potential loss, and apoptosis. IKKβ-IN-7 inhibits phosphorylation of p65 and IκBα, suppresses p65 nuclear translocation, and regulates NF-κB-controlled genes. IKKβ-IN-7 suppresses tumor growth in xenograft models and shows activity against colorectal cancer with low normal cell cytotoxicity. IKKβ-IN-7 can be used for the research of colorectal cancer[1].

IC50 & Target[1]

IKKβ

9.44 μM (IC50)

p65

 

Bax

 

Bcl-2

 

Bcl-xL

 

体外研究
(In Vitro)

IKKβ-IN-7 (6i2) (给药 24 小时) 可强效抑制多种癌细胞系的增殖，包括 A549 细胞 (IC50 = 5.11 μM)、HepG2 细胞 (IC50 = 9.81 μM)、HCT-116 细胞 (IC50 = 1.08 μM)、HT-29 细胞 (IC50 = 4.17 μM)、RKO 细胞 (IC50 = 4.72 μM) 以及 CT-26 细胞 (IC50 = 0.86 μM)，同时对永生化人肝上皮正常细胞 THLE-2 的细胞毒性较低 (IC50 > 16 μM)[1]。
IKKβ-IN-7 (给药 1 小时) 可直接抑制 IKKβ 激酶活性，其 IC50 为 9.44 μM[1]。
IKKβ-IN-7 (2.0 μM; 30 min) 可强效抑制 Topo I 活性，在 37°C 孵育 30 min 后，2.0 μM 浓度下的抑制率达 96.84%[1]。
IKKβ-IN-7 (0.5-2.0 μM; 24 h) 在体外以剂量依赖的方式对 HCT-116 细胞产生多种生物学效应：通过增加 γ-H2AX 表达诱导 DNA 损伤并降低 Topo I 蛋白水平 (2.0 μM 时效果最强)；剂量依赖性地抑制 IκBα 和 p65 的磷酸化，从而抑制 NF-κB 通路的激活；抑制 p65 核转位而不改变 p65 总蛋白水平；调节 Bcl-2 家族蛋白的表达 (增加促凋亡蛋白 Bax 并降低抗凋亡蛋白 Bcl-2、Bcl-xl 和 Mcl-1)，表明诱导线粒体介导的细胞凋亡；在 2.0 μM 时诱导细胞凋亡，凋亡率为 68.29%；在 2.0 μM 浓度下可诱导 S 期细胞周期阻滞；增加细胞内 ROS 水平；降低线粒体膜电位[1]。
IKKβ-IN-7 (0.5-2.0 μM; 24 h, 48 h) 可呈剂量依赖性抑制人结直肠癌 HCT-116 细胞的伤口愈合迁移[1]。

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

IKKβ-IN-7 相关抗体:

Western Blot Analysis[1]

Cell Line: human colorectal carcinoma HCT-116 cells
Concentration: 0.5, 1, 2.0 μM
Incubation Time: 24 h
Result: Decreased Topo I levels by more than 50% at 2.0 μM, and increased γ-H2AX expression by 2–3-fold in a dose-dependent manner compared with untreated controls.
Reduced the phosphorylation levels of IκBα and p65 gradually to less than 0.5-fold of control levels as concentration increased from 0.5 to 2.0 μM.
Left total p65 protein levels unchanged, but decreased nuclear p65 levels significantly and increased cytoplasmic p65 levels in a dose-dependent manner compared with controls.
Increased Bax expression in a dose-dependent manner, while significantly reduced the expression of anti-apoptotic proteins Bcl-2, Bcl-xL and Mcl-1 in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: human colorectal carcinoma HCT-116 cells
Concentration: 0.5, 1, 2.0 μM
Incubation Time: 24 h
Result: Induced apoptosis rates of 39.45% (0.5 μM), 58.14% (1.0 μM), and 68.29% (2.0 μM), compared to 8.86% in untreated controls.

Cell Cycle Analysis[1]

Cell Line: human colorectal carcinoma HCT-116 cells
Concentration: 0.5, 1, 2.0 μM
Incubation Time: 24 h
Result: Induced S-phase arrest, with the proportion of cells in S phase reaching 44.6% at 2.0 μM, in a dose-dependent manner.

Cell Migration Assay[1]

Cell Line: human colorectal carcinoma HCT-116 cells
Concentration: 0.5, 1, 2.0 μM
Incubation Time: 24 h; 48 h
Result: Inhibited wound healing in a dose-dependent manner, with wound healing rates of 25.23% (24 h, 0.5 μM), 5.70% (24 h, 1.0 μM), 4.69% (24 h, 2.0 μM), 69.67% (48 h, 0.5 μM), 54.78% (48 h, 1.0 μM), and 18.35% (48 h, 2.0 μM), compared to 43.05% (24 h) and 94.61% (48 h).
体内研究
(In Vivo)

IKKβ-IN-7 (6i2) (2.5-60 mg/kg；腹腔注射；每 2 天 1 次，连续 2 天) 在 CT-26 异种移植模型中显示出显著的体内抗肿瘤功效，且安全性良好、急性毒性低，同时具有一定的血浆稳定性并能持续释放 SN-38 (HY-13704)[1]。

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

Animal Model: Female immunocompetent BALB/c mice (5-6 weeks old) were subcutaneously injected with CT-26 cells (3 × 106 cells per mouse in 100 μL sterile PBS)[1]
Dosage: 2.5 mg/kg, 5 mg/kg
Administration: Intraperitoneal (IP) injection; once every other day
Result: Exhibited potent antitumor efficacy with tumor growth inhibition (TGI) rates of 68.81% (2.5 mg/kg) and 95.41% (5 mg/kg).
No significant body weight loss or animal mortality observed during the treatment period.
H&E staining of major organs (heart, liver, spleen, lung, kidney) revealed no obvious morphological abnormalities.
Superior safety profile compared to 10-HCPT (which caused inflammatory cell infiltration in spleen and glomerular atrophy in kidney at 2.5 mg/kg).
Animal Model: Female immunocompetent BALB/c mice (20.0 g) were used for acute toxicity test[1]
Dosage: 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg, 60 mg/kg
Administration: Intraperitoneal (IP) injection; once daily; each dose administered for 2 consecutive days (total 12 days)
Result: No animal death observed at doses up to 20 mg/kg.
Minimal lethal dose (MLD) and median lethal dose (LD50) were determined based on survival status, with lower toxicity than 10-HCPT (which caused mortality at 5 mg/kg).
分子量

786.82

Formula

C45H42N2O11
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-7 相关分类

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  • 稀释计算器

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  • 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-73117527-92-8IKKNF-κBBcl-2 FamilyReactive Oxygen Species (ROS)ApoptosisIκB kinaseI kappa B kinase Nuclear factor-κBNuclear factor-kappaBTopo ICT-26 cellsIκBαcolorectal cancerp65IKKβHCT-116 cellsTHLE-2 cellsapoptosisInhibitorinhibitorinhibit

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