2. Metabolic Enzyme/Protease Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Cathepsin Apoptosis PARP Caspase
  4. Cathepsin-IN-5

Cathepsin-IN-5 是一种组织蛋白酶 (cathepsin) 抑制剂，对组织蛋白酶 L (cathepsin L) 和组织蛋白酶 S (cathepsin S) 的 IC50 值分别为 6.2 μM 和 81 nM。Cathepsin-IN-5 可抑制癌细胞增殖、诱导细胞凋亡 (apoptosis)、降低小鼠模型中肝细胞肿瘤的生长，并调控与细胞死亡、细胞增殖及细胞过程相关的基因表达。Cathepsin-IN-5 可用于肝细胞癌的研究。

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Cathepsin-IN-5

Cathepsin-IN-5 Chemical Structure

CAS No. : 2475078-38-5

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Cathepsin-IN-5 相关抗体

Top Publications Citing Use of Products

查看 Cathepsin 亚型特异性产品:

查看所有亚型
Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cathepsin-IN-5 is a cathepsin inhibitor with IC50 values of 6.2 μM and 81 nM for cathepsin L and cathepsin S. Cathepsin-IN-5 inhibits cancer cells proliferation, induces apoptosis, reduces growth of hepatocellular tumors in mouse models, and modulates expression of genes linked to cell death, cell proliferation, and cellular processes. Cathepsin-IN-5 can be used for the research of hepatocellular carcinoma[1].

IC50 & Target[1]

cathepsin S

81 nM (IC50)

cathepsin L

6.2 μM (IC50)

PARP1

 

Caspase 3

 

体外研究
(In Vitro)

Cathepsin-IN-5 (Compound 1) (0.15-300 μM; 24-72 h) 对 Hep G2 和 Hep 3B 肝癌细胞系表现出时间依赖性抗增殖活性，其 IC50 值范围为 1.8 至 6.4 μM[1]。
Cathepsin-IN-5 (7.5-10 μM; 72-96 h) 在伤口愈合实验中可抑制 Hep G2 细胞的迁移与增殖[1]。
Cathepsin-IN-5 (0.1-50 μM; 2-24 h) 以浓度和时间依赖的方式抑制 Hep G2 细胞裂解物中内组织蛋白酶 L (IC50 = 6.2 μM) 和组织蛋白酶 S (IC50 = 81 nM) 的活性[1]。
Cathepsin-IN-5 (0.1-50 μM; 2.5-24 h) 不会在 Hep G2 或 Hep 3B 细胞中诱导显著的细胞内 ROS 生成[1]。
Cathepsin-IN-5 (5-20 μM; 1-24 h) 可在 Hep G2 细胞中诱导呈浓度和时间依赖性的基因表达变化，富集与巨自噬、细胞凋亡及细胞迁移相关的通路[1]。
Cathepsin-IN-5 (5-20 μM; 6-24 h) 可显著上调 Hep G2 细胞中 sqstm1、gabarapl1、akr1c1 和 akap12 的表达[1]。
Cathepsin-IN-5 (5-20 μM; 6-24 h) 可以浓度和时间依赖的方式激活 Hep G2 细胞的凋亡，并升高剪切型 PARP1 和剪切型 caspase-3 水平[1]。

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

Cathepsin-IN-5 相关抗体:

Real Time qPCR[1]

Cell Line: Hep G2
Concentration: 5, 20 μM
Incubation Time: 6 h; 24 h
Result: Significantly upregulated sqstm1, gabarapl1, and akr1c1 expression at 5 μM and 20 μM after 6 h.
Significantly upregulated sqstm1, gabarapl1, akr1c1, and akap12 expression at 20 μM after 24 h.
Modestly decreased angptl8 expression at 20 μM after 24 h.

Western Blot Analysis[1]

Cell Line: Hep G2
Concentration: 5, 20 μM
Incubation Time: 6 h; 24 h
Result: Increased cleaved PARP1 levels at 20 μM after 6 h and 24 h.
Increased cleaved caspase-3 levels at 5 μM and 20 μM after 6 h and 24 h.
Showed concentration- and time-dependent increases in cleaved PARP1 and cleaved caspase-3 levels.
体内研究
(In Vivo)

Cathepsin-IN-5 (Compound 1) (100-150 mg/kg；皮下注射；每日一次；连续 15 天) 可抑制裸鼠皮下 HCC 异种移植物的生长[1]。

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

Animal Model: Foxn1nu (immunocompromised, subcutaneous Hep 3B2.1−7 xenograft model)[1]
Dosage: 100 mg/kg; 150 mg/kg
Administration: s.c.; daily; 15 days (administered proximal to the tumor)
Result: Resulted in a tumor volume fold increase of ~1 (100 mg/kg) and ~2 (150 mg/kg), compared to ~7 in vehicle-treated mice.
Did not significantly elevate plasma AST and ALT levels relative to vehicle-treated mice.
Showed no significant difference in BUN and creatinine levels from vehicle controls.
Showed no signs of systemic toxicity (e.g., lethargy, weight loss).
分子量

440.47

Formula

C22H20N2O6S
CAS 号
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-IN-5 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-IN-52475078-38-5CathepsinApoptosisPARPCaspasepoly ADP ribose polymeraseapoptosishuman cathepsin Lcell deathmacroautophagyHep G2mouse modelsHep 3Bcell proliferationhuman cathepsin Shepatocellular carcinoma cellsInhibitorinhibitorinhibit

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