Proteases are essential enzymes that break down proteins by cleaving peptide bonds, playing a crucial role in various physiological processes, including digestion, immune response, and cell signaling. Dysregulation of protease activity is associated with numerous diseases, such as cancer, cardiovascular disorders, and neurodegenerative diseases.
Recent years have witnessed substantial progress in the development of protease inhibitors. These advancements are driven by a better understanding of protease structure and function, as well as innovations in drug design and screening technologies. However, one of the primary challenges in protease research is the accurate measurement of enzyme activity, which is critical for the identification and validation of potential inhibitors.
Our service leverages Fluorescence Intensity (FI) to deliver precise and reliable measurements of protease activity. Protease, when active, recognize and cleave a specific peptide sequence at a certain site. The short peptide used in the assay contains this recognition sequence and a fluorescent tag. Upon cleavage, the fluorescent tag is separated from the peptide, resulting in an increase in fluorescence that can be measured. The higher the fluorescence value, the higher the protease activity, indicating the efficiency of the protease in cleaving its substrate.
| Target | Synonyms | Reference Compound | Assay Format |
|---|---|---|---|
| Neutrophil Elastase | ELA2, ELANE | Sivelestat | FI |
| Chymotrypsin C | ELA4, CTRC | Chymostatin | FI |
| Plasminogen | plasmin | ZK824859 | FI |
| u-Plasminogen Activator | Urokinase, uPA | UK-371804 | FI |
| t-Plasminogen Activator | Reteplase, tPA | ZK824859 | FI |
| Trypsin 2 | PRSS2, TRYP2 | BMS-262084 | FI |
| DPP3 | / | Spinorphin TFA | FI |
| DPP4 | CD26 | Linagliptin | FI |
| DPP7 | DPP2, QPP | Talabostat | FI |
| DPP8 | DPRP1 | 1G244 | FI |
| DPP9 | DPRP2 | 1G244 | FI |
| Coagulation Factor II | Thrombin | Dabigatran | FI |
| Coagulation Factor VII | SPCA | PCI-27483 | FI |
| Coagulation Factor Xa | Stuart Factor | Edoxaban | FI |
| Coagulation Factor XI | PTA | Asundexian | FI |
| Coagulation Factor XIIa | / | Nafamostat (mesylate) | FI |
| Coagulation Factor XIV | Protein C, APC | Nafamostat | FI |
| TMPRSS2 | PRSS10 | Camostat | FI |
| Furin | PCSK3 | SSM3 | FI |
| Kallikrein 1 | KLK1 | Avoralstat | FI |
| Kallikrein 2 | KLK2 | Avoralstat | FI |
| Kallikrein 4 | KLK4 | Avoralstat | FI |
| Kallikrein 5 | KLK5 | Avoralstat | FI |
| Kallikrein 6 | KLK6 | Avoralstat | FI |
| Kallikrein 8 | KLK8 | Avoralstat | FI |
| Kallikrein 11 | KLK11 | Avoralstat | FI |
| Kallikrein 12 | KLK12 | Avoralstat | FI |
| Kallikrein 13 | KLK13 | Avoralstat | FI |
| Kallikrein 14 | KLK14 | Avoralstat | FI |
| Plasma Kallikrein | KLKB1, PPK | Avoralstat | FI |
| Cathepsin B | CTSB, APPS | Leupeptin | FI |
| Cathepsin C | CTSC, DPP1, PALS | AZD7986 | FI |
| Cathepsin G | CTSG | CTSG inhibitor I | FI |
| Cathepsin H | ACC-4, ACC-5, aleurain | E-64 | FI |
| Cathepsin K | CTSK, CTSO, CTSO2 | Odanacatib | FI |
| Cathepsin L | CTSL, CTSL1 | SID-26681509 | FI |
| Cathepsin S | CTSS | LY-3000328 | FI |
| Cathepsin V | Cathepsin L2, CTSL2 | E-64 | FI |
| Cathepsin X | CTSX, CTSZ | Leupeptin | FI |
| 3CL Protease | Mpro | PF-07311332 | FI |
| Papain-like Protease | Plpro, pp1a | GRL0617 | FI |
| MALT1 | PCASP1, MLT1, IMD12 | MLT-748 | FI |
| AEP | Legumain | RR-11a | FI |
| Cathepsin D | CTSD | Pepstatin | FI |
| Cathepsin E | CTSE | Pepstatin | FI |
| Renin | REN | Aliskiren | FI |
| BACE-1 | ASP2, beta-secretase 1 | LY2886721 | FI |
| MMP-1 | CLGN | Ilomastat | FI |
| MMP-2 | CLG4, Gelatinase A | Ilomastat | FI |
| MMP-3 | STR1, stromelysin-1 | Ilomastat | FI |
| MMP-7 | Matrilysin, PUMP-1 | Batimastat | FI |
| MMP-8 | Collagenase 2, PMNL-CL | XL-784 | FI |
| MMP-9 | Gelatinase B, GELB | Ilomastat | FI |
| MMP-10 | Stromelysin 2, transin 2 | Ilomastat | FI |
| MMP-12 | Macrophage elastase | UK-370106 | FI |
| MMP-13 | CLG3 | XL-784 | FI |
| MMP-14 | MT1-MMP | Marimastat | FI |
| MMP-15 | SMCP-2 | Ilomastat | FI |
| MMP-16 | MMP-X2 | Ilomastat | FI |
| IDE | / | ML345 | FI |
| PSMA | FOLH1, GCP2 | PSMA-617 | FI |
| ACE | CD143, DCP | Captopril | FI |
| ACE2 | ACEH | MLN-4760 | FI |
| Aminopeptidase A | ENPEP, APACD249 | RB150 | FI |
| ERAP1 | Aminopeptidase PILS, ARTS1 | ERAP1-IN-1 | FI |
| Complement Component C1s | C1 esterase, C1S | BCX-1470 | FI |
| APN | Aminopeptidase N | Bestatin | FI |
| QPCT | Glutaminyl-peptide cyclotransferase | SEN177 | FI |
| FAP | / | PT-100 | FI |
| Caspase 1 | CASP1, IL1BC, IL1BCE | Belnacasan | FI |
| Caspase 2 | CASP2, ICH1, NEDD2 | Ac-DEVD-CHO | FI |
| Caspase 3 | CASP3, CPP32 | Ac-DEVD-CHO | FI |
| Caspase 4 | CASP4, ICH2 | Belnacasan | FI |
| Caspase 6 | CASP6, MCH2 | Ac-DEVD-CHO | FI |
| Caspase 7 | CASP7, MCH3 | Ac-DEVD-CHO | FI |
| Caspase 8 | CASP8, MCH5 | Ac-DEVD-CHO | FI |
| Caspase 10 | CASP10, MCH4 | Ac-DEVD-CHO | FI |
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