Cathepsin L Inhibitor Screening Kit (Fluorometric) (197012) is an assay that uses the ability of active Cathepsin L to cleave the synthetic AFC-based peptide substrate to release AFC, which can be easily quantified using a fluorometer or fluorescence microplate reader.
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- Nature communications 14:10762023Identification of SARS-CoV-2 M inhibitors containing P1' 4-fluorobenzothiazole moiety highly active against SARS-CoV-2.Applications:Unspecified applicationReactive species:Unspecified reactive speciesNobuyo Higashi-Kuwata,Kohei Tsuji,Hironori Hayashi,Haydar Bulut,Maki Kiso,Masaki Imai,Hiromi Ogata-Aoki,Takahiro Ishii,Takuya Kobayakawa,Kenta Nakano,Nobutoki Takamune,Naoki Kishimoto,Shin-Ichiro Hattori,Debananda Das,Yukari Uemura,Yosuke Shimizu,Manabu Aoki,Kazuya Hasegawa,Satoshi Suzuki,Akie Nishiyama,Junji Saruwatari,Yukiko Shimizu,Yoshikazu Sukenaga,Yuki Takamatsu,Kiyoto Tsuchiya,Kenji Maeda,Kazuhisa Yoshimura,Shun Iida,Seiya Ozono,Tadaki Suzuki,Tadashi Okamura,Shogo Misumi,Yoshihiro Kawaoka,Hirokazu Tamamura,Hiroaki MitsuyaPubMed 36841831
- European journal of medicinal chemistry 244:1148032022Discovery of novel SARS-CoV-2 3CL protease covalent inhibitors using deep learning-based screen.Applications:Unspecified applicationReactive species:Unspecified reactive speciesLiying Wang,Zhongtian Yu,Shiwei Wang,Zheng Guo,Qi Sun,Luhua LaiPubMed 36209629
- European journal of medicinal chemistry 238:1145082022Discovery of 2-(furan-2-ylmethylene)hydrazine-1-carbothioamide derivatives as novel inhibitors of SARS-CoV-2 main protease.Applications:Unspecified applicationReactive species:Unspecified reactive speciesXiaodong Dou,Qi Sun,Guofeng Xu,Yameng Liu,Caifang Zhang,Bingding Wang,Yangbin Lu,Zheng Guo,Lingyu Su,Tongyu Huo,Xinyi Zhao,Chen Wang,Zhongtian Yu,Song Song,Liangren Zhang,Zhenming Liu,Luhua Lai,Ning JiaoPubMed 35688005
- Theranostics 11:9821-98322021CST6 protein and peptides inhibit breast cancer bone metastasis by suppressing CTSB activity and osteoclastogenesis.Applications:Unspecified applicationReactive species:Unspecified reactive speciesXiaoxun Li,Yajun Liang,Cheng Lian,Fangli Peng,Yansen Xiao,Yunfei He,Chengxin Ma,Yuan Wang,Peiyuan Zhang,Yuhan Deng,Yunpeng Su,Cheng Luo,Xiangyin Kong,Qingcheng Yang,Tong Liu,Guohong HuPubMed 34815788
- Biological & pharmaceutical bulletin 40:1240-12462017Design, Synthesis, and Structure-Activity Relationship Study of Epoxysuccinyl-Peptide Derivatives as Cathepsin B Inhibitors.Applications:Unspecified applicationReactive species:Unspecified reactive speciesXiaoye Zhang,Xiaohong Yang,Hongqiang Wang,Song Li,Kun Guo,Dan Jiang,Junhai Xiao,Di LiangPubMed 28502922
Key facts
- Detection method
Fluorescent
- Sample types
Inhibitor compounds
- Assay type
Quantitative
Target data
Function
Thiol protease important for the overall degradation of proteins in lysosomes (Probable). Plays a critical for normal cellular functions such as general protein turnover, antigen processing and bone remodeling. Involved in the solubilization of cross-linked TG/thyroglobulin and in the subsequent release of thyroid hormone thyroxine (T4) by limited proteolysis of TG/thyroglobulin in the thyroid follicle lumen (By similarity). In neuroendocrine chromaffin cells secretory vesicles, catalyzes the prohormone proenkephalin processing to the active enkephalin peptide neurotransmitter (By similarity). In thymus, regulates CD4(+) T cell positive selection by generating the major histocompatibility complex class II (MHCII) bound peptide ligands presented by cortical thymic epithelial cells. Also mediates invariant chain processing in cortical thymic epithelial cells (By similarity). Major elastin-degrading enzyme at neutral pH. Accumulates as a mature and active enzyme in the extracellular space of antigen presenting cells (APCs) to regulate degradation of the extracellular matrix in the course of inflammation (By similarity). Secreted form generates endostatin from COL18A1 (PubMed:10716919). Critical for cardiac morphology and function. Plays an important role in hair follicle morphogenesis and cycling, as well as epidermal differentiation (By similarity). Required for maximal stimulation of steroidogenesis by TIMP1 (By similarity).Isoform 2Functions in the regulation of cell cycle progression through proteolytic processing of the CUX1 transcription factor (PubMed:15099520). Translation initiation at downstream start sites allows the synthesis of isoforms that are devoid of a signal peptide and localize to the nucleus where they cleave the CUX1 transcription factor and modify its DNA binding properties (PubMed:15099520).(Microbial infection) Facilitates human coronaviruses SARS-CoV and SARS-CoV-2 infections via proteolysis of coronavirus spike (S) glycoproteins in lysosome for entry into host cell (PubMed:32142651, PubMed:32221306, PubMed:16339146, PubMed:18562523). Proteolysis within lysosomes is sufficient to activate membrane fusion by coronaviruses SARS-CoV and EMC (HCoV-EMC) S as well as Zaire ebolavirus glycoproteins (PubMed:16081529, PubMed:26953343, PubMed:18562523).
Alternative names
Procathepsin L, Cathepsin L1, Major excreted protein, MEP, CTSL1, CTSL
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Cathepsin L Inhibitor Screening Kit (Fluorometric) (197012) is an assay that uses the ability of active Cathepsin L to cleave the synthetic AFC-based peptide substrate to release AFC, which can be easily quantified using a fluorometer or fluorescence microplate reader.
Alternative names
Procathepsin L, Cathepsin L1, Major excreted protein, MEP, CTSL1, CTSL
Key facts
- Detection method
Fluorescent
- Sample types
Inhibitor compounds
- Assay type
Quantitative
- Assay Platform
Microplate reader
Storage
- Shipped at conditions
Blue Ice
- Appropriate short-term storage conditions
-20°C
- Appropriate long-term storage conditions
-20°C
- Storage information
-20°C
Notes
Cathepsin L Inhibitor Screening Kit (Fluorometric) (197012) is an assay that uses the ability of active Cathepsin L to cleave the synthetic AFC-based peptide substrate to release AFC, which can be easily quantified using a fluorometer or fluorescence microplate reader. In the presence of a Cathepsin L inhibitor, the cleavage of this substrate is reduced/abolished resulting in decrease or total loss of the AFC fluorescence. This simple and high-throughput adaptable assay kit can be used to screen/study/characterize potential inhibitors of Cathepsin L.
This product is manufactured by BioVision, an Abcam company and was previously called K161 Cathepsin L Inhibitor Screening Kit (Fluorometric). K161-100 is the same size as the 100 test size of ab197012.
Cathepsin L (CTSL, EC 3.4.22.15) is a lysosomal cysteine protease that is implicated in protein degradation, arthritis, apoptosis, and cancer. Cathepsin L plays a major role in antigen processing, tumor invasion and metastasis, bone resorption, and turnover of intracellular and secreted proteins involved in growth regulation. Although commonly recognized as a lysosomal protease, cathepsin L is also secreted. This broad-spectrum protease is potent in degrading several extracellular proteins (laminins, fibronectin, collagens I and IV, elastin, and other structural proteins of basement membranes) as well as serum proteins and cytoplasmic and nuclear proteins.
Supplementary info
This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
Cathepsin L also known as major excreted protein (MEP) or EC 3.4.22.15 is a critical cysteine protease with a molecular weight of approximately 30-40 kDa. It performs proteolytic functions within the lysosomes executing the breakdown of proteins into peptides. This protease expresses prominently in various tissues including liver kidney spleen and lungs where it fulfills tasks integral to cellular maintenance and turnover.
- Biological function summary
This protease contributes to antigen processing and the degradation of intracellular proteins. Cathepsin L participates in essential processes such as protein catabolism and the remodeling of the extracellular matrix. Although it is not part of a large protein complex its enzymatic activity influences multiple cellular functions making it an active agent in maintaining cellular homeostasis.
- Pathways
Cathepsin L takes part in the antigen processing and presentation pathway contributing to immune system functions. It also associates with the lysosomal pathway for protein degradation interacting with other cathepsins such as Cathepsin B and Cathepsin D. These pathways place it centrally in maintaining protein balance within cells and its activity can affect various downstream cellular processes.
- Associated diseases and disorders
Cathepsin L has associations with cancer and neurodegenerative disorders. Its overexpression can lead to increased invasiveness and metastasis in various cancers due to enhanced proteolytic activity. It also relates to Alzheimer's disease where abnormal protease function can disrupt the processing of amyloid precursor protein contributing to amyloid beta aggregation. In these conditions cathepsin L functions in concert with proteins like Cathepsin B linking it to pathological processes.
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Functional Studies - Cathepsin L Inhibitor Assay Kit (Fluorometric) (ab197012)
Inhibition of Cathepsin L activity by Cathepsin L inhibitor.
Inhibition of Cathepsin L activity using CTSL (cathepsin L inhibitor) provided in the kit. Assay was performed following the kit protocol.
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