MAPK-IN-8
MAPK-IN-8 is an orally active MAPK inhibitor. MAPK-IN-8 can restore the balance of gut microbiota, inhibit M1 macrophage polarization and suppress MAPK mediated inflammation. MAPK-IN-8 can be used in ulcerative colitis research.
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- Formule: C15H18BrN3OS
- Masse moléculaire:368.29
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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p38 |
iNOS |
COX-2 |
ERK |
IL-6 |
TNF-α |
Claudin-1 |
JNK |
MAPK-IN-8 (compound 20) (20 µM; 24 h) exhibits no significant toxicity toward RAW 264.7 cells[1].
MAPK-IN-8 (20 µM; pretreatment for 4 h + co-incubation with LPS (HY-D1056) (100 ng/mL for 12 h) significantly inhibits nitric oxide (NO) production in RAW 264.7 cells with an inhibition rate of 67.64%. MAPK-IN-8 significantly downregulates the protein and mRNA expression levels of LPS-induced inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in RAW 264.7 cells. MAPK-IN-8 reduces the secretion of the pro-inflammatory cytokines TNF-α and IL-6 [1].
MAPK-IN-8 (20 µM; pretreatment for 4 h + co-incubation with LPS (100 ng/mL) + IFN-γ (20 ng/mL) for 12 h) modulates macrophage polarization in RAW 264.7 cells. MAPK-IN-8 almost completely blocks polarization toward pro-inflammatory M1 macrophages while actively promoting polarization toward anti-inflammatory M2 macrophages[1].
MAPK-IN-8 (5-20 µM; pretreatment for 4 h + co-incubation with LPS (100 ng/mL for 12 h) inhibits the overactivation of the MAPK signaling pathway in RAW 264.7 cells. MAPK-IN-8 significantly reduces the phosphorylation levels of key components of the MAPK cascade (p38, JNK and ERK) in a dose-dependent manner[1].
MAPK-IN-8 (20 µM; pretreatment for 4 h + co-incubation with exposure to macrophage-conditioned medium for 16 h) significantly protects Caco2 intestinal epithelial cells against the degradation and disruption of tight junction proteins (ZO-1, Occludin, Claudin-4) induced by inflammatory mediators[1].
MAPK-IN-8 (> 128 µg/mL) does not exhibit direct antibacterial activity against various Gram-negative pathogenic bacteria (Escherichia coli, Salmonella typhimurium, Klebsiella pneumoniae and Acinetobacter baumannii) (MIC > 128 µg/mL)[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 cells
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Concentration:20 µM
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Incubation Time:Pretreatment for 4 h + co-incubation with LPS (100 ng/mL) for 12 h
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Result:Significantly downregulated NO, iNOS and COX-2 protein levels in RAW 264.7 cells.
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Cell Line:RAW 264.7 cells
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Concentration:20 µM
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Incubation Time:24 h
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Result:Showed no obvious toxicity to RAW 264.7 cells.
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Cell Line:RAW 264.7 cells
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Concentration:20 µM
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Incubation Time:Pretreatment for 4 h + co-incubation with LPS (100 ng/mL) for 12 h
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Result:Significantly downregulated iNOS and COX-2 mRNA levels in RAW 264.7 cells.
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Cell Line:RAW 264.7 cells
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Concentration:20 µM
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Incubation Time:Pretreatment for 4 h + co-incubation with LPS (100 ng/mL) for 12 h
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Result:Reduced the secretion of the pro-inflammatory cytokines TNF-α and IL-6.
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Cell Line:RAW 264.7 cells
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Concentration:5 µM, 10 µM, 20 µM
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Incubation Time:Pretreatment for 4 h + co-incubation with LPS (100 ng/mL) for 12 h
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Result:Significantly reduced the phosphorylation levels of key components of the MAPK cascade (p38, JNK and ERK) in a dose-dependent manner.
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Cell Line:Caco2 cells
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Concentration:20 µM
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Incubation Time:Pretreatment for 4 h + co-incubation with exposure to macrophage-conditioned medium for 16 h
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Result:Inhibited the degradation and disruption of tight junction proteins (ZO-1, Occludin, Claudin-4) in Caco2 cells.
MAPK-IN-8 (200 mg/kg or 300 mg/kg; i.g.; once daily; for 3 days) shows excellent gastrointestinal safety in fasted male Wistar rat models[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 mice (7-weeks-old, female) were fed with 2% DSS for 7 days[1].
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Dosage:10 mg/kg
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Administration:i.g.; once daily; for 7 days
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Result:Significantly ameliorated weight loss, colon shortening and disease activity index (DAI) scores.
Protected and maintained the expression of intestinal epithelial tight junction proteins (ZO-1, Occludin, Claudin-4).
Significantly suppressed the accumulation of M1 macrophages in the colon and spleen and the production of pro-inflammatory mediators (INOS, TNF-α, IL-6 and MPO) in vivo.
Inhibited the phosphorylation of MAPK signaling pathways (ERK, JNK and p38).
Reshaped the disrupted gut microbiota.
Showed no apparent toxic side effects on major organs such as the heart, liver, spleen, lungs and kidneys.
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Animal Model:Wistar rats (220-270 g, male) were fasted for 18 h[1].
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Dosage:10 mg/kg
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Administration:i.g.; once daily; for 3 days
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Result:Did not induce severe ulcers larger than 3 mm, and compared to the corresponding doses of IBU, its ulcer index (UI) was reduced by 90.3% and 78.4%.
Exhibited no significant inhibitory effect on COX-1 protein expression in the gastric mucosa, thereby avoiding the severe depletion of protective prostaglandin E2 (PGE2).
Chemical Information
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Masse moléculaire 368.29
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Formule C15H18BrN3OS
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SMILES
CC(C1=CC=C(CC(C)C)C=C1)C(NC2=NN=C(Br)S2)=O
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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)
MAPK-IN-8 Related Classifications
HY-184744 Related Classifications
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