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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- Formule: C18H14Cl2N4O
- Masse moléculaire:373.24
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
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ERK5 403.4 nM (IC50) |
Bax |
Bcl-2 |
Caspase-3 |
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.
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Cell Line:Human non-small cell lung cancer A549 cells
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Concentration:20-80 μM
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Incubation Time:48 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 20-25 g, subcutaneous inoculation with Lewis lung carcinoma cells)[1]
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Dosage:12.5 mg/kg; 25 mg/kg
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Administration:p.o.; 9 consecutive days
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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.
Chemical Information
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Masse moléculaire 373.24
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Formule C18H14Cl2N4O
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SMILES
O=C(C1=CC=CC(Cl)=C1Cl)N(CC2)CC=C2C3=CNC4=NC=NC=C43
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ERK5-IN-7 Related Classifications
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