2. NF-κB Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. NF-κB Interleukin Related c-Kit
  4. Anti-inflammatory agent 117

Anti-inflammatory agent 117 is an orally active anti-inflammatory agent and c-Kit kinase inhibitor with an IC50 of 15.2 μM. Anti-inflammatory agent 117 blocks the NF-κB signaling pathway and inhibits the release of IL-6. Anti-inflammatory agent 117 exhibits anti-inflammatory effects in mouse models of acute lung injury, sepsis and ulcerative colitis. Anti-inflammatory agent 117 can be used in research related to acute lung injury, sepsis and ulcerative colitis.

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Anti-inflammatory agent 117

Anti-inflammatory agent 117 Chemical Structure

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Anti-inflammatory agent 117 Related Antibodies

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Description

Anti-inflammatory agent 117 is an orally active anti-inflammatory agent and c-Kit kinase inhibitor with an IC50 of 15.2 μM. Anti-inflammatory agent 117 blocks the NF-κB signaling pathway and inhibits the release of IL-6. Anti-inflammatory agent 117 exhibits anti-inflammatory effects in mouse models of acute lung injury, sepsis and ulcerative colitis. Anti-inflammatory agent 117 can be used in research related to acute lung injury, sepsis and ulcerative colitis[1].

IC50 & Target[1]

IL-6

 

In Vitro

Anti-inflammatory agent 117 (Compound z18) (10 μM; 30 min pretreatment followed by 24 h LPS stimulation) potently inhibits LPS-induced IL-6 release in J774A.1 macrophages, with an inhibition rate of 78.55% at the concentration of 10 μM[1].
Anti-inflammatory agent 117 (10 μM; 24 h) exhibits low cytotoxicity in J774A.1 macrophages[1].
Anti-inflammatory agent 117 (10 μM; 2 h) inhibits the activation of the NF-κB signaling pathway in LPS-stimulated J774A.1 macrophages by maintaining IκBα levels and reducing p-p65 levels[1].
Anti-inflammatory agent 117 (10-100000 nM) moderately inhibits c-Kit kinase activity in cell-free biochemical assays, with an IC50 of 15.2 μM[1].
Anti-inflammatory agent 117 (treated at 37°C for 2-8 h) exhibits good 8-hour stability in rat serum, simulated gastric fluid and enzyme-free simulated intestinal fluid at 37°C, and only undergoes moderate degradation in enzyme-containing simulated intestinal fluid (with a residual concentration of approximately 55% after 8 h)[1].

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

Anti-inflammatory agent 117 Related Antibodies
In Vivo

Anti-inflammatory agent 117 (20 mg/kg; p.o.) significantly attenuates LPS-induced acute lung injury in mice by reducing pulmonary edema, inflammatory cell infiltration, and inflammatory cytokine production at both the protein and mRNA levels[1].
Anti-inflammatory agent 117 (20 mg/kg; p.o.) improves survival outcomes and reduces weight loss in mice with LPS-induced sepsis[1].
Anti-inflammatory agent 117 (20 mg/kg; p.o.; daily; 10 days) significantly ameliorates DSS-induced ulcerative colitis in mice by reducing weight loss, colon shortening, splenomegaly, systemic inflammation, and histopathological tissue damage[1].

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

Animal Model: C57BL/6 (male, 19-23 g, intratracheal LPS-induced acute lung injury)[1]
Dosage: 20 mg/kg
Administration: p.o.; single dose 30 minutes prior to LPS challenge
Result: Significantly reduced the lung wet/dry ratio compared to the LPS group.
Significantly decreased total protein concentration and total cell count in BALF compared to the LPS group.
Significantly reduced BALF levels of IL-6 and TNF-α compared to the LPS group.
Significantly reduced serum levels of IL-6 and TNF-α compared to the LPS group.
Reduced lung tissue neutrophil and macrophage infiltration, attenuated pulmonary edema, congestion, and alveolar wall thickening.
Significantly lowered lung tissue mRNA levels of IL-6, TNF-α, and IL-1β compared to the LPS group.
Animal Model: C57BL/6 (intraperitoneal LPS-induced sepsis)[1]
Dosage: 20 mg/kg
Administration: p.o.; single dose 1 hour prior to LPS challenge
Result: Delayed mortality (deaths occurring between 36 and 60 hours) with a subset surviving until the end of the 10-day observation period, while all mice in the LPS group died between 24 and 36 hours.
Slowed the rate of weight loss in septic mice, with body weight stabilizing after 60 hours.
Animal Model: C57BL/6 (2.5% DSS-induced ulcerative colitis)[1]
Dosage: 20 mg/kg
Administration: p.o.; daily; 10 days
Result: Reduced DSS-induced body weight loss, partially restoring weight after DSS withdrawal.
Increased colon length to 7.6 cm (compared to 5.8 cm in the DSS model group).
Reduced spleen weight to near normal control levels.
Maintained a significantly lower DAI score throughout the experimental period compared to the DSS model group.
Significantly reduced serum IL-6 levels compared to the DSS model group.
Attenuated histopathological damage in colon (reduced goblet cell loss, crypt necrosis, and mucosal destruction) and spleen (reduced white pulp fusion and red pulp macrophage infiltration), as well as suppressed inflammatory cell infiltration in colon tissue.
Molecular Weight

551.62

Formula

C30H25N5O4S
SMILES

O=C(C(C(NC1=CC(C)=C(OC2=CC=NC(C(NCCC3=CC=CS3)=O)=C2)C=C1)=O)=N4)C=CN4C5=CC=CC=C5
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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Anti-inflammatory agent 117 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:

Anti-inflammatory agent 117NF-κBInterleukin Relatedc-KitNuclear factor-κBNuclear factor-kappaBILSCFRCD117NF-κB signaling pathwayRAW264.7 macrophagessepsismacrophagesIκBαinterleukin-6J774A.1 macrophagesacute lung injuryc-Kit kinaseulcerative colitisInhibitorinhibitorinhibit

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