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

Anti-inflammatory agent 113 (compound B5) 是一种组织蛋白酶 L (CTSL)抑制剂与抗炎剂，其 CTSL IC50 为 5.52 μM。Anti-inflammatory agent 113 可抑制 CTSL 的成熟，减弱 NF-κB 和 p38 MAPK 信号通路的激活，并通过与 Asp162、Cys25 和 Glu63 的非共价相互作用稳定结合于 CTSL 的活性位点。Anti-inflammatory agent 113 可抑制促炎细胞因子 (IL-6、IL-8) 的产生，减少炎症细胞的肺浸润，缓解肺组织损伤。Anti-inflammatory agent 113 可用于急性肺损伤的研究。

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Anti-inflammatory agent 113

Anti-inflammatory agent 113 Chemical Structure

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Anti-inflammatory agent 113 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Anti-inflammatory agent 113 (compound B5) (0.30-10 μM; 30 min pretreatment, 24 h LPS incubation) 可强效且呈剂量依赖性地抑制 LPS 诱导的 HBE 细胞中 IL-6 (IC50 = 2.51 μM) 和 IL-8 (IC50 = 1.15 μM) 的产生[1]。
Anti-inflammatory agent 113 (0.30-10 μM; 30 min pretreatment, 24 h LPS incubation) 可强效且呈剂量依赖性地抑制 LPS 诱导的 THP-1 细胞中 IL-6 (IC50 = 0.76 μM) 和 IL-8 (IC50 = 4.06 μM) 的产生[1]。
Anti-inflammatory agent 113 (0.30-10 μM; 30 min pretreatment, 24 h LPS incubation) 可强效且呈剂量依赖性地抑制 Raw 264.7 细胞中 LPS 诱导的 IL-6 产生，其 IC50 为 0.73 μM[1]。
Anti-inflammatory agent 113 (0.625-5 μM; 30 min pretreatment, 16 h LPS stimulation) 可浓度依赖性地抑制 LPS 诱导的人支气管上皮细胞 (HBE cells) 中 CTSL 的成熟[1]。
Anti-inflammatory agent 113 (0.625-5 μM; 30 min pretreatment, 16 h LPS stimulation) 可浓度依赖性地抑制 LPS 诱导的 HBE 细胞中 NF-κB 和 p38 MAPK 信号通路的激活[1]。
Anti-inflammatory agent 113 (0.001-100 μM; 30 min) 可强效抑制 CTSL 酶活性，其 IC50 为 5.52 μM[1]。

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

Anti-inflammatory agent 113 相关抗体:

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.
体内研究
(In Vivo)

Anti-inflammatory agent 113 (10-20 mg/kg; i.p.; daily; 3 days) 可通过减少炎症细胞浸润、细胞因子产生和肺水肿，显著减轻雄性 C57BL/6 小鼠中 LPS 诱导的急性肺损伤[1]。

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.
分子量

448.52

Formula

C27H24N6O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Anti-inflammatory agent 113 相关分类

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  • 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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