2. MAPK/ERK Pathway Stem Cell/Wnt Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. ERK Apoptosis Bcl-2 Family Caspase Reactive Oxygen Species (ROS)
  4. ERK5-IN-7

ERK5-IN-7 是一种口服有效的 ERK5 抑制剂，IC50 为 403.4 nM。ERK5-IN-7 可直接抑制 ERK5 激酶活性，下调 ERK5 的磷酸化水平及总蛋白表达。ERK5-IN-7 可诱导凋亡 (Apoptosis) (上调 Bax，下调 Bcl-2，诱导 Caspase-3 裂解)。ERK5-IN-7 诱导 ROS 积聚。 ERK5-IN-7 对 Lewis 肺癌具有抗癌作用。

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ERK5-IN-7

ERK5-IN-7 Chemical Structure

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ERK5-IN-7 相关抗体

Top Publications Citing Use of Products

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ERK5-IN-7 is an orally active ERK5 inhibitor with an IC50 of 403.4 nM. ERK5-IN-7 directly inhibits ERK5 kinase activity, and downregulates the phosphorylation level and total protein expression of ERK5. ERK5-IN-7 induces Apoptosis (upregulates Bax, downregulates Bcl-2, and induces Caspase-3 cleavage). ERK5-IN-7 induces ROS accumulation. ERK5-IN-7 exhibits anticancer effects against Lewis lung cancer[1].

IC50 & Target[1]

ERK5

403.4 nM (IC50)

Bax

 

Bcl-2

 

Caspase-3

 

体外研究
(In Vitro)

ERK5-IN-7 可强效抑制纯化的重组 ERK5 激酶活性，其 IC50 为 403.4 nM[1]。
ERK5-IN-7 (20 μg/mL; 48 h) 可抑制人非小细胞肺癌 A549 细胞的增殖，处理 48 h 后其 IC50 为 40.1 μM[1]。
ERK5-IN-7 (20-80 μM; 48 h) 呈浓度依赖性地抑制 A549 细胞中 ERK5 磷酸化及总 ERK5 蛋白的表达[1]。
ERK5-IN-7 (20-80 μM; 48 h) 以浓度依赖方式通过内源性线粒体通路诱导 A549 细胞凋亡[1]。

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

ERK5-IN-7 相关抗体:

Apoptosis Analysis[1]

Cell Line: Human non-small cell lung cancer A549 cells
Concentration: 20-80 μM
Incubation Time: 48 h
Result: Increased the apoptotic rate from 7.7% (control) to 79.8%.
Upregulated pro-apoptotic Bax expression.
Downregulated anti-apoptotic Bcl-2 expression.
Induced caspase-3 cleavage.
体内研究
(In Vivo)

ERK5-IN-7 (12.5-25 mg/kg；口服；连续 9 天) 在 Lewis 肺癌小鼠模型中具有抗癌作用[1]。

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

Animal Model: C57BL/6 (male, 20-25 g, subcutaneous inoculation with Lewis lung carcinoma cells)[1]
Dosage: 12.5 mg/kg; 25 mg/kg
Administration: p.o.; 9 consecutive days
Result: Achieved a 30.8% tumor growth inhibition rate at 12.5 mg/kg.
Achieved a 49.3% tumor growth inhibition rate at 25 mg/kg.
Showed no significant changes in mouse body weight throughout the treatment period.
Downregulated ERK5 expression in tumor tissues.
Upregulated the pro-apoptotic protein Bax in tumor tissues.
Downregulated the anti-apoptotic protein Bcl-2 in tumor tissues.
Reduced Ki67-positive cells in tumor tissues.
Caused no observable pathological alterations in major organs (heart, liver, spleen, lungs, kidneys) compared to controls.
分子量

373.24

Formula

C18H14Cl2N4O
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

ERK5-IN-7 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:

ERK5-IN-7ERKApoptosisBcl-2 FamilyCaspaseReactive Oxygen Species (ROS)Extracellular signal regulated kinasesreactive oxygen speciescancer cellsmitochondrial apoptotic pathwaynon-small cell lung cancerhuman ERK5A549 cellsendoplasmic reticulum stressLewis lung carcinoma mouse modelmitochondrial dysfunctionERK5Inhibitorinhibitorinhibit

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