JNK2/MKK7 PPI-IN-1
JNK2/MKK7 PPI-IN-1 is an orally active JNK2 inhibitor with an IC50 of 0.99 μM and a Kd of 81.6 μM. JNK2/MKK7 PPI-IN-1 inhibits JNK2 kinase activity, disrupts JNK2-MKK7 protein-protein interaction, and reduces c-Jun phosphorylation. JNK2/MKK7 PPI-IN-1 inhibits LPS-induced overexpression of inflammatory cytokines IL-6 and TNF-α. JNK2/MKK7 PPI-IN-1 can be used for the research of acute lung injury.
For research use only. We do not sell to patients.
- Formula: C26H25N3O5
- Molecular Weight:459.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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JNK2 0.99 μM (IC50) |
JNK2 81.6 μM (Kd) |
IL-6 |
JNK2/MKK7 PPI-IN-1 (6I) (0.08-10 μM; 24 h) inhibits LPS-induced IL-6 secretion in J774A.1 macrophages (IC50 = 2.78 μM) and THP-1 macrophages (IC50 = 0.14 μM), and suppresses TNF-α secretion in J774A.1 macrophages (IC50 = 0.55 μM)[1].
JNK2/MKK7 PPI-IN-1 (5, 10 μM; 24 h) suppresses LPS-induced IL-6 and TNF-α mRNA expression in RAW 264.7 macrophages[1].
JNK2/MKK7 PPI-IN-1 (0.125-4 μM) inhibits JNK2 kinase activity with an IC50 of 0.99 μM[1].
JNK2/MKK7 PPI-IN-1 (20-60 μM) disrupts the interaction between JNK2 and MKK7, as confirmed by co-immunoprecipitation assays[1].
JNK2/MKK7 PPI-IN-1 (6.25-200 μM) binds to JNK2 with a Kd of 81.6 μM, measured by surface plasmon resonance (SPR)[1].
JNK2/MKK7 PPI-IN-1 (10 μM; 1 h) stabilizes JNK2 protein against thermal denaturation in intact RAW 264.7 cells[1].
JNK2/MKK7 PPI-IN-1 (0.2-5 μM; 24 h) inhibits LPS-induced phosphorylation of c-Jun, p38, and p65, and preserves IκBα protein level in RAW 264.7 macrophages[1].
JNK2/MKK7 PPI-IN-1 (5 μM; 24 h) suppresses LPS-induced nuclear translocation of c-Jun in RAW 264.7 macrophages, visualized by immunofluorescence staining[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW 264.7 macrophages
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Concentration:10 μM (pre-incubation for LPS-induced IL-6 inhibition); 0.08, 0.4, 2, 10 μM (dose-response testing)
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Incubation Time:0.5 h (pre-incubation); 24 h (LPS stimulation)
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Result:Inhibited LPS-induced IL-6 production by 86.86% at 10 μM, with an IC50 of 0.32 μM in a dose-dependent manner.
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Cell Line:RAW 264.7 macrophages
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Concentration:5, 10 μM
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Incubation Time:3 h (pre-incubation); 6 h (LPS stimulation)
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Result:Significantly suppressed LPS-induced elevations in IL-6 and TNF-α mRNA levels in a dose-dependent manner.
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Cell Line:RAW 264.7 macrophages
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Concentration:10 μM
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Incubation Time:2 h (pre-incubation); 30 min (LPS stimulation)
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Result:Significantly suppressed LPS-induced nuclear translocation of c-Jun.
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Cell Line:RAW 264.7 macrophages
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Concentration:0.2 μM, 1 μM, 5 μM
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Incubation Time:2 h (pre-incubation); 30 min (LPS stimulation)
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Result:Inhibits LPS-induced phosphorylation of c-Jun, p38, and p65; preserves IκBα protein level compared to LPS-treated group.
JNK2/MKK7 PPI-IN-1 (500 mg/kg; p.o.; single dose) shows favorable acute safety in male C57BL/6 mice, with no mortality, organ damage, or persistent body weight loss[1].
JNK2/MKK7 PPI-IN-1 (100 mg/kg; p.o.; daily; 14 days) shows favorable subacute safety in male C57BL/6 mice, with no mortality, organ damage, or significant liver enzyme elevation[1].
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, 18-22 g, LPS-induced ALI)[1]
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Dosage:20 mg/kg
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Administration:p.o.; three doses at 12-hour intervals
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Result:Significantly attenuated LPS-induced pulmonary edema (reduced lung wet/dry weight ratio).
Decreased protein concentration and total cell counts in bronchoalveolar lavage fluid (BALF).
Reduced IL-6 levels in both serum and BALF.
Alleviated LPS-induced splenomegaly.
Reduced lung tissue damage, neutrophil influx, and macrophage infiltration compared to LPS-only controls.
Reduced splenic histopathological changes compared to LPS-only controls.
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Animal Model:C57BL/6 (male, 18-22 g, CLP-induced sepsis ALI)[1]
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Dosage:20 mg/kg
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Administration:p.o.; three doses at 12-hour intervals
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Result:Significantly reduced CLP-induced pulmonary edema (lower lung wet/dry weight ratio compared to CLP-only controls).
Decreased protein concentration and total cell counts in BALF.
Reduced IL-6 and IL-1β levels in BALF.
Ameliorated CLP-induced splenomegaly.
Reduced lung tissue injury, inflammatory cell infiltration, and alveolar septal thickening compared to CLP-only controls.
Reduced splenic white pulp fusion compared to CLP-only controls.
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Animal Model:C57BL/6 (male, 18-22 g)[1]
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Dosage:500 mg/kg
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Administration:p.o.; single dose
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Result:Observed no mortality or abnormal behaviors.
Showed an initial slight decrease in body weight, followed by gradual recovery to levels comparable to controls.
Showed no significant organ damage in heart, liver, spleen, lung, or kidney tissues via histopathological analysis.
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Animal Model:C57BL/6 (male, 18-22 g)[1]
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Dosage:100 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Observed no mortality or abnormal behaviors.
Showed a non-significant decrease in body weight that recovered by day 6.
Showed no significant differences in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels compared to controls.
Showed no significant organ damage in heart, liver, spleen, lung, or kidney tissues via histopathological analysis.
Chemical Information
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Molecular Weight 459.49
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Formula C26H25N3O5
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SMILES
O=C(NC1=CC=C(OC2=CC=NC3=CC(OC(C)C)=C(C=C32)OC)C=C1)C4=CN(C(C=C4)=O)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JNK2/MKK7 PPI-IN-1 Related Classifications
HY-181812 Related Classifications
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