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

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.

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ERK5-IN-7

ERK5-IN-7 Chemical Structure

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ERK5-IN-7 Related Antibodies

Top Publications Citing Use of Products

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ERK ERK1 ERK2 ERK5 ERK8

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

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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

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Description

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

 

In Vitro

ERK5-IN-7 (serially diluted concentrations; 10 min pre-incubation at 25 °C, 60 min at 25 °C) potently inhibits purified recombinant human ERK5 kinase activity with an IC50 of 403.4 nM[1].
ERK5-IN-7 (20 μg/mL; 48 h) inhibits A549 human non-small cell lung cancer cell proliferation with an IC50 of 40.1 μM after 48 h of treatment[1].
ERK5-IN-7 (20-80 μM; 48 h) concentration-dependently suppresses phosphorylated and total ERK5 protein expression in A549 cells after 48 h of treatment[1].
ERK5-IN-7 (20-80 μM; 48 h) concentration-dependently induces apoptosis in A549 cells via the intrinsic mitochondrial pathway, including Bax upregulation, Bcl-2 downregulation, and caspase-3 activation, after 48 h of treatment[1].

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

ERK5-IN-7 Related Antibodies

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.
In Vivo

ERK5-IN-7 (12.5-25 mg/kg; p.o.; for 9 consecutive days) exhibits anticancer activity in a mouse model of Lewis lung cancer[1].

MedChemExpress (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.
Molecular Weight

373.24

Formula

C18H14Cl2N4O
SMILES

O=C(C1=CC=CC(Cl)=C1Cl)N(CC2)CC=C2C3=CNC4=NC=NC=C43
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ERK5-IN-7 Related Classifications

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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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