2. Metabolic Enzyme/Protease
  3. Cathepsin
  4. Cathepsin D degrader 1

Anti-hepatic fibrosis agent 3 是一种靶向 Cathepsin D 的口服活性抗肝纤维化化合物。Anti-hepatic fibrosis agent 3 对 COL1A1-promoter 的 IC50 为 53.18 μM，与 Cathepsin D 结合的 Kd 为 8.86 μM。Anti-hepatic fibrosis agent 3 可直接结合并促进 Cathepsin D 的降解，对 Cathepsin B 或 Cathepsin L 无显著作用。Anti-hepatic fibrosis agent 3 可抑制肝星状细胞活化，减少细胞外基质沉积及炎症细胞因子的表达。Anti-hepatic fibrosis agent 3 在大鼠 BDL 和小鼠 CDAHFD 诱导的肝纤维化模型中表现出显著的抗纤维化活性。Anti-hepatic fibrosis agent 3 可用于肝纤维化的研究。

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Cathepsin D degrader 1

Cathepsin D degrader 1 Chemical Structure

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Cathepsin D degrader 1 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-hepatic fibrosis agent 3 is an orally active anti-hepatic fibrosis compound targeting Cathepsin D. Anti-hepatic fibrosis agent 3 shows an IC50 of 53.18 μM against COL1A1-promoter and a Kd of 8.86 μM for binding to Cathepsin D. Anti-hepatic fibrosis agent 3 directly binds to and promotes the degradation of Cathepsin D, with no significant effect on Cathepsin B or Cathepsin L. Anti-hepatic fibrosis agent 3 inhibits hepatic stellate cell activation and reduces extracellular matrix deposition and inflammatory cytokine expression. Anti-hepatic fibrosis agent 3 exhibits remarkable anti-fibrotic activity in rat BDL and mouse CDAHFD-induced hepatic fibrosis models. Anti-hepatic fibrosis agent 3 can be used for the study of hepatic fibrosis[1].

IC50 & Target[1]

Cathepsin D

8.86 μM (Kd)

体外研究
(In Vitro)

Anti-hepatic fibrosis agent 3 (compound 9a) 可强效抑制 LX-2 细胞中 COL1A1 启动子的活性，其 IC50 为 53.18 μM，选择性指数为 3.60[1]。
Anti-hepatic fibrosis agent 3 (20-80 μM; 24 h) 可抑制 TGFβ1 诱导的 LX-2 细胞中纤维化标志物蛋白 (COL1A1、纤连蛋白、α-SMA、p-Smad2) 的表达，并下调纤维化相关基因的 mRNA 水平 (COL1A1、纤连蛋白、TGFB1、MMP2、ACTA2、TIMP1)，且以浓度依赖的方式降低小鼠肝星状细胞 (mHSC) 中纤维化相关蛋白的表达[1]。
Anti-hepatic fibrosis agent 3 (20-80 μM; 24 h) 可呈剂量依赖性下调 LX-2 和 mHSC 细胞中 pro-Cathepsin D 与 Cathepsin D 的蛋白水平，但对 Cathepsin B 和 Cathepsin L 无影响；同时可降低经 Lipopolysaccharides (HY-D1056) 刺激的 LX-2 和 mHSC 细胞中炎症蛋白 (IL-1β、caspase-1) 的表达[1]。
Anti-hepatic fibrosis agent 3 (80 μM; 6-48 h) 可加速经 Cycloheximide (HY-12320) 预处理的 LX-2 细胞中前组织蛋白酶 D 和组织蛋白酶 D 的降解[1]。

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

Cathepsin D degrader 1 相关抗体:

RT-PCR[1]

Cell Line: LX-2 cells
Concentration: 20 μM, 40 μM, 80 μM
Incubation Time: 24 h
Result: Dose-dependently downregulates the mRNA levels of fibrosis-related genes (COL1A1, fibronectin, TGFB1, MMP2, ACTA2, TIMP1).

Western Blot Analysis[1]

Cell Line: Cycloheximide (CHX)-pretreated LX-2 cells
Concentration: 80 μM
Incubation Time: 6 h, 12 h, 24 h, 36 h, 48 h
Result: Significantly accelerated the degradation of pro-Cathepsin D and Cathepsin D.

Western Blot Analysis[1]

Cell Line: LPS-stimulated LX-2 cells, LPS-stimulated mHSC
Concentration: 20 μM, 40 μM, 80 μM
Incubation Time: 24 h
Result: Significantly decreased the protein levels of inflammatory factors IL-1β and caspase-1.

Western Blot Analysis[1]

Cell Line: LX-2 cells, mouse hepatic stellate cells (mHSC)
Concentration: 20 μM, 40 μM, 80 μM
Incubation Time: 24 h
Result: Dose-dependently downregulated the protein levels of Cathepsin D, pro-Cathepsin D, COL1A1, fibronectin, α-SMA and p-Smad2, and showed no significant effect on Cathepsin B and Cathepsin L.

Western Blot Analysis[1]

Cell Line: TGFβ1-stimulated LX-2 cells
Concentration: Anti-hepatic fibrosis agent 3 (20 μM, 40 μM, 80 μM), L-theanine (20 μM, 40 μM, 80 μM)
Incubation Time: 24 h
Result: Dose-dependently downregulates fibrosis-related proteins (COL1A1, fibronectin, α-SMA, p-Smad2, MMP2, TGFβ1, CTGF, TIMP1); exhibits stronger inhibitory activity than L-theanine and most tested analogs.
体内研究
(In Vivo)

Anti-hepatic fibrosis agent 3 (100-200 mg/kg; p.o.; daily; 14 days) 可剂量依赖性地缓解雄性 Sprague-Dawley 大鼠中 BDL 诱导的肝纤维化与炎症，在 100 mg/kg 和 200 mg/kg 剂量下可显著降低血清肝损伤标志物水平、胶原沉积量、纤维化及炎症生物标志物的表达量，以及 Cathepsin D 水平[1]。
Anti-hepatic fibrosis agent 3 (100-200 mg/kg; p.o.; daily; 4 weeks) 可剂量依赖性地改善 C57BL/6 小鼠中由 CDAHFD 诱导的代谢性肝纤维化与炎症；在 100 mg/kg 和 200 mg/kg 剂量下，其可显著改善血清肝损伤标志物水平、减少胶原沉积、降低纤维化及炎症生物标志物的表达，并下调组织蛋白酶 D 水平[1]。

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

Animal Model: Sprague-Dawley (male, 180-200 g, BDL surgery-induced hepatic fibrosis)[1]
Dosage: 100 mg/kg; 200 mg/kg
Administration: p.o.; daily; 14 days
Result: Significantly reduced serum levels of aspartate aminotransferase (AST), lactate dehydrogenase (LDH), and total bilirubin (TBIL) in a dose-dependent manner.
Improved liver elasticity and surface smoothness compared to BDL model group.
Reduced liver injury and collagen deposition in a dose-dependent manner via histological analysis; significantly reduced hepatic necrosis at 200 mg/kg dose.
Significantly reduced liver hydroxyproline content in 200 mg/kg dose group.
Downregulated protein levels of fibrotic biomarkers (Fibronectin, COL1A1, α-SMA, TGFβ1, CTGF, TIMP1) in liver tissue in a dose-dependent manner.
Downregulated mRNA levels of Col1a1 and Acta2 in 200 mg/kg dose group.
Reduced protein levels of pro-Cathepsin D and Cathepsin D in liver tissue in a dose-dependent manner.
Inhibited protein and mRNA expression of pro-inflammatory factors (IL-6, IL-1β) and reduced inflammation score in pathological sections in a dose-dependent manner.
Animal Model: C57BL/6 (8-week-old, CDAHFD feeding-induced hepatic fibrosis)[1]
Dosage: 100 mg/kg; 200 mg/kg
Administration: p.o.; daily; 4 weeks
Result: Improved serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), and total bilirubin (TBIL) in a dose-dependent manner, with greater efficacy than positive control OCA for ALT and ALP.
Partially restored hepatic luster and elasticity compared to CDAHFD model group.
Reduced hepatic ballooning degeneration and collagen deposition via histological analysis; reduced hepatic fibrosis scores in a dose-dependent manner via semiquantitative scoring.
Significantly reduced liver hydroxyproline content in both dose groups.
Downregulated protein levels of fibrotic biomarkers (COL1A1, Fibronectin, α-SMA) and mRNA levels of Col1a1, Mmp2, Timp1, and Acta2 in liver tissue.
Reduced protein levels of pro-Cathepsin D and Cathepsin D in liver tissue in a dose-dependent manner.
Inhibited protein and mRNA expression of pro-inflammatory factor (IL-6) in a dose-dependent manner.
分子量

368.47

Formula

C22H28N2O3
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

Cathepsin D degrader 1 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:

Cathepsin D degrader 1Cathepsin D degrader1Cathepsin D degrader-1CathepsinCathepsin DSprague-Dawley ratsmHSC cellshepatic fibrosisKM miceTGFβ1Cathepsin Lhepatic stellate cellsCathepsin BLX-2 cellsInhibitorinhibitorinhibit

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