2. Metabolic Enzyme/Protease
  3. Cathepsin
  4. Anti-inflammatory agent 113

Anti-inflammatory agent 113 (compound B5) is a Cathepsin L (CTSL) inhibitor and anti-inflammatory agent with a CTSL IC50 of 5.52 μM. Anti-inflammatory agent 113 suppresses CTSL maturation, attenuates NF-κB and p38 MAPK signaling pathway activation, and binds stably in CTSL’s active site via noncovalent interactions with Asp162, Cys25, and Glu63. Anti-inflammatory agent 113 inhibits pro-inflammatory cytokine (IL-6, IL-8) production, reduces inflammatory cell lung infiltration, and alleviates lung tissue injury. Anti-inflammatory agent 113 can be used for the research of acute lung injury.

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Anti-inflammatory agent 113

Anti-inflammatory agent 113 Chemical Structure

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Anti-inflammatory agent 113 Related Antibodies

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Description

Anti-inflammatory agent 113 (compound B5) is a Cathepsin L (CTSL) inhibitor and anti-inflammatory agent with a CTSL IC50 of 5.52 μM. Anti-inflammatory agent 113 suppresses CTSL maturation, attenuates NF-κB and p38 MAPK signaling pathway activation, and binds stably in CTSL’s active site via noncovalent interactions with Asp162, Cys25, and Glu63. Anti-inflammatory agent 113 inhibits pro-inflammatory cytokine (IL-6, IL-8) production, reduces inflammatory cell lung infiltration, and alleviates lung tissue injury. Anti-inflammatory agent 113 can be used for the research of acute lung injury[1].

In Vitro

Anti-inflammatory agent 113 (compound B5) (0.30-10 μM; 30 min pretreatment, 24 h LPS incubation) potently and dose-dependently inhibits LPS-induced IL-6 (IC50 = 2.51 μM) and IL-8 (IC50 = 1.15 μM) production in HBE cells[1].
Anti-inflammatory agent 113 (0.30-10 μM; 30 min pretreatment, 24 h LPS incubation) potently and dose-dependently inhibits LPS-induced IL-6 (IC50 = 0.76 μM) and IL-8 (IC50 = 4.06 μM) production in THP-1 cells[1].
Anti-inflammatory agent 113 (0.30-10 μM; 30 min pretreatment, 24 h LPS incubation) potently and dose-dependently inhibits LPS-induced IL-6 production in Raw 264.7 cells with an IC50 of 0.73 μM[1].
Anti-inflammatory agent 113 (0.625-5 μM; 30 min pretreatment, 16 h LPS stimulation) concentration-dependently inhibits LPS-induced CTSL maturation in HBE cells[1].
Anti-inflammatory agent 113 (0.625-5 μM; 30 min pretreatment, 16 h LPS stimulation) concentration-dependently inhibits LPS-induced activation of the NF-κB and p38 MAPK signaling pathways in HBE cells[1].
Anti-inflammatory agent 113 (0.001-100 μM; 30 min) potently inhibits CTSL enzymatic activity with an IC50 of 5.52 μM[1].

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

Anti-inflammatory agent 113 Related Antibodies

ELISA Assay[1]

Cell Line: human bronchial epithelial (HBE) cells
Concentration: 0.30-10 μM
Incubation Time: 30 min (pretreatment); 24 h (LPS incubation)
Result: Exhibited dose-dependent inhibition of IL-6 and IL-8 production, with IC50 values of 2.51 μM for IL-6 and 1.15 μM for IL-8.

ELISA Assay[1]

Cell Line: Raw 264.7 cells
Concentration: 0.30-10 μM
Incubation Time: 30 min (pretreatment); 24 h (LPS incubation)
Result: Inhibited IL-6 production with an IC50 value of 0.73 μM.

Western Blot Analysis[1]

Cell Line: HBE cells
Concentration: 0.625-5 μM
Incubation Time: 30 min (pretreatment); 16 h (LPS stimulation)
Result: Inhibited LPS-induced CTSL maturation in a clear, concentration-dependent manner.\nReduced LPS-induced levels of phospho-IκBα, phospho-p65, and phospho-p38, indicating suppression of NF-κB and p38 MAPK pathway activation.
In Vivo

Anti-inflammatory agent 113 (10-20 mg/kg; i.p.; daily; 3 days) significantly attenuates LPS-induced acute lung injury in male C57BL/6 mice by reducing inflammatory cell infiltration, cytokine production, and pulmonary edema[1].

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

Animal Model: C57BL/6 (male, 20-25 g)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; daily; 3 days
Result: Significantly reduced inflammatory cell infiltration in lung tissue and preserved alveolar architecture compared to the LPS-only group at 10 mg/kg and 20 mg/kg.
Significantly suppressed LPS-induced increases in IL-6 and TNF-α levels in bronchoalveolar lavage fluid (BALF), reduced total cell counts and total protein concentrations in BALF, and decreased the lung wet-to-dry weight ratio at 20 mg/kg.
Downregulated LPS-induced CTSL expression in mouse lung tissue.
Molecular Weight

448.52

Formula

C27H24N6O
SMILES

O=C(NC1=CC=CC(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)=C1)[C@@H](N)CC5=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 113 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 113CathepsinAsp162THP-1 cellsp38 MAPK signaling pathwayGlu63Cys25NF-κBIL-6IL-8HBE cellsCathepsin L (CTSL)Inhibitorinhibitorinhibit

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