Protease Assay Services
Proteases are targeted successfully for the treatment of HIV and Hepatitis C. Inhibitors have been approved for the treatment of hypertension (ACE inhibitors), Diabetes (DPP-IV inhibitor), and to prevent blood clots (Factor Xa inhibitors). Studies are also underway for the treatment of Alzheimer's, COVID-19, and cancer.
Our panel of protease assays provides a platform for profiling and selectivity screening of new protease inhibitors against all major classes of proteases, such as serine proteases, cysteine proteases, threonine proteases, aspartic proteases, glutamic proteases, and metalloproteases. Selective compounds can be further characterized via both biochemical and biophysical platforms, such as surface plasmon resonance for their kinetic profile and mechanism of action on a molecular level.
- Fluorescence-based activity assay
- Low and large scale screening as well as high-throughput screening options are available
- Full protease panel screening is performed on a monthly basis
- Discover our new COVID-19-related protease assays here
List of Targets
| Name | HGNC Symbol | Additional Synonyms | Data |
|---|---|---|---|
| ACE1 | ACE | Angiotensin-converting enzyme | Data sheet |
| ACE2 | ACE2 | angiotensin I converting enzyme 2 | Please inquire |
| ADAM10 | ADAM10 | a disintegrin and metalloproteinase domain 10, MADM HsT18717 CD156C | Please inquire |
| BACE1 | BACE1 | Beta-secretase 1 | Data sheet |
| Calpain1 | CPN1 | - | Please inquire |
| Caspase1 | CASP1 | Interleukin-1 beta convertase, p45, IL1BC, IL1BCE | Data sheet |
| Caspase10 | CASP10 | ICE-like apoptotic protease 4, Apoptotic protease Mch-4, FAS-associated death domain protein interleukin-1B-converting enzyme 2, FLICE2 | Data sheet |
| Caspase11 | n.a. | mouse Caspase 4, Protease ICH-3, CASP4, Casp11, Caspl, Ich3 | Data sheet |
| Caspase14 | CASP14 | CASPE | Data sheet |
| Caspase2 | CASP2 | Neural precursor cell expressed developmentally down-regulated protein 2, Protease ICH-1, ICH1, NEDD2 | Data sheet |
| Caspase3 | CASP3 | Apopain, Cysteine protease CPP32, Protein Yama, SREBP cleavage activity 1, CPP32 | Data sheet |
| Caspase4 | CASP4 | ICE(rel)-II, Protease ICH-2, Protease TX, ICH2 | Data sheet |
| Caspase5 | CASP5 | ICE(rel)-III, Protease ICH-3, Protease TY, ICH3 | Data sheet |
| Caspase6 | CASP6 | Apoptotic protease Mch-2, MCH2 | Data sheet |
| Caspase7 | CASP7 | Apoptotic protease Mch-3, CMH-1, ICE-like apoptotic protease 3, MCH3 | Data sheet |
| Caspase8 | CASP8 | Apoptotic cysteine protease, Apoptotic protease Mch-5, CAP4, FADD-homologous ICE/ced-3-like protease, FADD-like ICE, ICE-like apoptotic protease 5, MORT1-associated ced-3 homolog, MCH5 | Data sheet |
| Caspase9 | CASP9 | Apoptotic protease Mch-6, Apoptotic protease-activating factor 3, ICE-like apoptotic protease 6, MCH6 | Data sheet |
| Cathepsin B | CTSB | APP secretase, Cathepsin B1, CATB, CPSB | Data sheet |
| Cathepsin C | CTSC | DPP1, PLS, PALS | Please inquire |
| Cathepsin D | CTSD | CPSD, CATD | Data sheet |
| Cathepsin E | CTSE | CATE | Data sheet |
| Cathepsin G | CTSG | CG | Please inquire |
| Cathepsin H | CTSH | CPSB, ACC-4, ACC-5, ACC4, ACC5 | Please inquire |
| Cathepsin K | CTSK | Cathepsin O/O2/X | Data sheet |
| Cathepsin L | CTSL | CTSL1, MEP | Data sheet |
| Cathepsin S | CTSS | - | Please inquire |
| Cathepsin V | CTSV | CTSL2, cathepsin L2 | Please inquire |
| Chymase | CMA1 | - | Please inquire |
| Chymotrypsin | n.a. | Please inquire | |
| Dipeptidyl peptidase IV (DDP-IV) | DPP4 | ADCP2, CD26 | Please inquire |
| Dipeptidyl peptidase IX (DPPIX) | DPP9 | DPRP2 | Please inquire |
| Dipeptidyl peptidase VIII (DPPVIII) | DPP8 | DPRP1 | Please inquire |
| Elastase | ELANE | Bone marrow serine protease, Elastase-2, Human leukocyte elastase, Medullasin, ELA2 | Data sheet |
| Factor VIIa | F7 | Coagulation factor VII | Please inquire |
| Factor Xa | F10 | Coagulation factor X | Please inquire |
| Factor XIa | F11 | Coagulation factor XI, FXI | Please inquire |
| Furin | FURIN | FUR, PACE, PCSK3 | Data sheet |
| HIV Protease | n.a. | - | Please inquire |
| Kallikrein 1 | KLK1 | - | Please inquire |
| Kallikrein 12 | KLK12 | kallikrein related peptidase 12, KLK-L5 | Please inquire |
| Kallikrein 13 | KLK13 | kallikrein related peptidase 13, KLK-L4 | Please inquire |
| Kallikrein 14 | KLK14 | kallikrein related peptidase 14, KLK-L6 | Please inquire |
| Kallikrein 5 | KLK5 | kallikrein related peptidase 5, SCTE, KLK-L2 | Please inquire |
| Kallikrein 7 | KLK7 | kallikrein related peptidase 7, SCCE | Please inquire |
| Matriptase 2 | TMPRSS6 | Transmembrane protease serine 6 | Data sheet |
| MMP 1 | MMP1 | Matrix metalloproteinase-2, MMP-2, Gelatinase A, TBE-1 | Data sheet |
| MMP 10 | MMP10 | matrix metallopeptidase 10, STMY2 | Please inquire |
| MMP 12 | MMP12 | HME, Matrix metalloproteinase-12, MMP-12, Macrophage elastase, ME | Data sheet |
| MMP 13 | MMP13 | Matrix metalloproteinase-13, MMP-13 | Data sheet |
| MMP 14 | MMP14 | MMP-14, Membrane-type matrix metalloproteinase 1, MT-MMP 1, MTMMP1, Membrane-type-1 matrix metalloproteinase, MT1-MMP, MT1MMP, MMP-X1 | Data sheet |
| MMP 2 | MMP2 | Matrix metalloproteinase-2, MMP-2, Gelatinase A, TBE-1 | Data sheet |
| MMP 3 | MMP3 | Matrix metalloproteinase-3, MMP-3, Transin-1, SL-1 | Data sheet |
| MMP 7 | MMP7 | Pump-1 protease, Uterine metalloproteinase, Matrix metalloproteinase-7, MMP-7, Matrin | Data sheet |
| MMP 8 | MMP8 | matrix metallopeptidase 8, CLG1 | Please inquire |
| MMP 9 | MMP9 | MMP-9, 92 kDa type IV collagenase, 92 kDa gelatinase, Gelatinase B, GELB | Data sheet |
| Neprilysin | MME | matrix metalloendopeptidase, CALLA, CD10, NEP | Please inquire |
| Papain | n.a. | Please inquire | |
| Plasma Kallikrein | KLKB1 | Fletcher factor, kallikrein B1 | Please inquire |
| Proteinase A | n.a. | Please inquire | |
| Proteinase K | n.a. | Please inquire | |
| SARS-CoV-2 Mpro | n.a. | SARS-CoV-2 Main Protease, SARS-CoV-2 3C-like Proteinase, 3CLpro | Data sheet |
| SARS-CoV-2 PLpro | n.a. | SARS-CoV-2 Papain-like Protease, NS3 | Data sheet |
| TACE | ADAM17 | A disintegrin and metalloproteinase domain 17, TNF-alpha-converting enzyme, TNF-alpha convertase, Snake venom-like protease, CD156b antigen | Data sheet |
| Thrombin | F2 | coagulation factor II | Please inquire |
| Trypsin | PRSS1 | Trypsin-1 | Please inquire |
| Tryptase g1 | n.a. | Please inquire | |
| Urokinase | PLAU | plasminogen activator | Please inquire |
| TMPRSS2 | TMPRSS2 | Transmembrane protease serine 2, Serine protease 10, PRSS10, TMPS2 | Data sheet |
Assay Details
Assay procedure for MMP1. Internally quenched fluorescent peptide substrates contain a fluorophore (5-FAM) and a quencher (QXL 520). A fluorescence signal is generated upon peptide cleavage which is quantified for determination of protease activity.
Setups: Single-dose screening in duplicates or IC50 value determination with 5 or 10 concentrations. Other screening formats are available upon request.
Controls: No inhibitor (DMSO vehicle) control and for every assay, one target-specific control compound is tested in 10-dose IC50 format.
Turnaround time: 10 business days for standard projects. Expedited scheduling and data delivery can be arranged prior to the commencement of the studies.
Report: The raw data, % enzyme activity and control compound IC50 values will be reported in Excel format for single-dose assays. For IC50 orders, raw data, IC50 values, and curve fitting will be delivered in Excel format. Assay conditions, target, and substrate information are available upon request. Requirements for this information should be noted prior to the commencement of the study.
Screening facility: This assay is performed at our screening facility in Malvern, PA, US.
Compound requirements: In brief, for a standard project, 20ul of a 10mM DMSO stock or solid material is needed. Less material is needed for large scale screening. Please refer to our FAQs for information regarding compound preparation and shipping.
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