MNK1/2-IN-10
MNK1/2-IN-10 is an orally active, selective MNK1/MNK2 inhibitor, with an IC50 of 10.84 nM for MNK1 and an IC50 of 12.81 nM for MNK2. MNK1/2-IN-10 inhibits eIF4E phosphorylation, the NF-κB signaling pathway, macrophage polarization, oxidative stress and the production of pro-inflammatory cytokines. MNK1/2-IN-10 alleviates kidney and spleen damage in LPS (HY-D1056)-induced inflammatory mouse models. Anti-inflammatory agent 115 is applicable for research related to acute inflammation.
For research use only. We do not sell to patients.
- Formula: C25H24N6O3S2
- Molecular Weight:520.63
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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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MNK1 10.84 nM (IC50) |
MNK2 12.81 nM (IC50) |
MNK1/2-IN-10 (Compound 13) (48 h) shows low cytotoxicity in RAW 264.7, HEK293T, HUVECs and AML-12 cell lines, with IC50 values ranging from 24.25 to 77.56 μM after 48 h of incubation[1].
MNK1/2-IN-10 (1.25-10 μM; 24 h) inhibits LPS-induced expression of p-eIF4E and iNOS in RAW 264.7 cells in a concentration-dependent manner[1].
MNK1/2-IN-10 (1.25-10 μM; 4 h) concentration-dependently inhibits the LPS-induced expression of p-eIF4E in RAW 264.7 cells[1].
MNK1/2-IN-10 (1.25-10 μM; 24 h) inhibits LPS-induced release of IL-6, TNF-α and MCP-1 in RAW 264.7 cells in a concentration-dependent manner[1].
MNK1/2-IN-10 (1.25-10 μM; 24 h) inhibits lipopolysaccharide (LPS)-induced nitric oxide release in RAW 264.7 cells in a concentration-dependent manner, with the maximum inhibitory effect observed at 10 μM[1].
MNK1/2-IN-10 (10 μM; 24 h) inhibits LPS-induced iNOS expression in RAW 264.7 cells[1].
MNK1/2-IN-10 (1.25-10 μM; 12 h) inhibits LPS-induced activation of the NF-κB pathway in RAW 264.7 cells in a concentration-dependent manner in vitro[1].
MNK1/2-IN-10 (10 μM; 24 h) inhibits LPS-induced nuclear translocation of P65 in RAW 264.7 cells[1].
MNK1/2-IN-10 (2.5-10 μM; 13 h) reduces LPS-induced ROS production in RAW 264.7 cells in a concentration-dependent manner[1].
MNK1/2-IN-10 (10 μM; 14 h) inhibits LPS-induced ROS production in RAW 264.7 cells[1].
MNK1/2-IN-10 (2.5-10 μM; 24 h) restores GSH levels and enhances SOD activity in LPS-stimulated RAW 264.7 cells in a concentration-dependent manner in vitro[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
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Concentration:10 μM, 5 μM, 2.5 μM, 1.25 μM
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Incubation Time:24 h
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Result:Suppressed LPS-induced phosphorylation of eIF4E in a concentration-dependent manner, with maximal suppression at 10 μM.
Suppressed LPS-induced expression of iNOS in a concentration-dependent manner, with maximal suppression at 10 μM.
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Cell Line:RAW 264.7
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Concentration:10 μM, 5 μM, 2.5 μM, 1.25 μM
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Incubation Time:2 h (pretreatment); 2 h (LPS stimulation)
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Result:Inhibited LPS-induced p-eIF4E expression in a concentration-dependent manner, as shown by reduced green fluorescence intensity.
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Cell Line:RAW 264.7
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Concentration:10 μM, 5 μM, 2.5 μM, 1.25 μM
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Incubation Time:24 h
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Result:Inhibited LPS-induced secretion of IL-6 in a dose-dependent manner.
Inhibited LPS-induced secretion of TNF-α in a dose-dependent manner.
Inhibited LPS-induced secretion of MCP-1 in a dose-dependent manner.
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Cell Line:RAW 264.7
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Concentration:10 μM
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Incubation Time:24 h
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Result:Diminished iNOS signal in the cytoplasm of LPS-stimulated cells.
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Cell Line:RAW 264.7
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Concentration:10 μM, 5 μM, 2.5 μM, 1.25 μM
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Incubation Time:12 h
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Result:Inhibited LPS-induced phosphorylation of P65 in a concentration-dependent manner.
Inhibited LPS-induced phosphorylation of IκBα in a concentration-dependent manner.
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Cell Line:RAW 264.7
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Concentration:10 μM
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Incubation Time:12 h (pretreatment); 12 h (LPS stimulation)
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Result:Blocked LPS-triggered nuclear translocation of P65, with significantly reduced fluorescence intensity in the nucleus.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6−8 weeks old, 18−21 g, LPS-induced)[1]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 16 days
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Result:Significantly reduced LPS-induced kidney and spleen indices, with the 100 mg/kg dose showing the strongest effect.
Improved renal function, reducing serum creatinine and urea nitrogen levels; the 50 and 100 mg/kg doses showed greater improvement than the positive control dexamethasone.
Mitigated LPS-induced kidney pathological changes (tubular dilation, brush border necrosis, vacuolization, structural disruption) and spleen pathological changes (nuclear swelling, cellular edema, inflammatory infiltration, microcirculatory dysfunction).
Significantly reduced serum levels of pro-inflammatory cytokines TNF-α, IL-6, MCP-1, and IL-1β, with the 100 mg/kg dose showing the strongest suppression.
Significantly suppressed p-eIF4E expression and downregulated the M1 macrophage marker iNOS in kidney and spleen tissues, with the 100 mg/kg dose showing the strongest effect.
Restored antioxidant capacity by increasing glutathione and superoxide dismutase levels, and reduced lipid peroxidation by lowering malondialdehyde levels in tissues.
Chemical Information
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Molecular Weight 520.63
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Formula C25H24N6O3S2
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SMILES
O=C(N1CCN(S(CCC)(=O)=O)CC1)C2=CC=C(C3=NN4C(S3)=NC=C4C5=CC=C(C#N)C=C5)C=C2
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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)
MNK1/2-IN-10 Related Classifications
HY-182939 Related Classifications
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