TMPRSS2 Fluorogenic Assay Kit
The TMPRSS2 Fluorogenic Assay is a homogeneous assay that takes advantage of a specific fluorogenic substrate which emits fluorescence upon cleavage by the protease. Only one step is required to assess TMPRSS2 activity: TMPRSS2 protease is incubated with the fluorogenic substrate and fluorescence is measured using a plate reader (λex = 383 nm, λem = 455 nm). Camostat, a known TMPRSS2 inhibitor, is supplied as a protease inhibitor control.
Figure: Illustration of the principle behind the fluorogenic TMPRSS2 protease assay. The peptide substrate is labeled with a fluorophore on one end and an acceptor on the other end. The fluorescence emitted by the donor fluorophore is quenched due to the proximity of the acceptor in the intact peptide. The protease cleaves the peptide and generates a highly fluorescent peptide fragment.
Need us to run inhibitor screens or profile your compounds against TMPRSS2? Check out our Protease Screening Services or Coronavirus Services.
This product has been cited 8 times.
- Fluorescent plate reader capable of reading fluorescence at λex = 383±15 nm, λem = 455±15 nm
- Adjustable micropipettor and tips
- Rotating or rocker platform
Catalog # | Name | Amount | Storage |
TMPRSS2* | 15 µg | -80°C | |
78047 | TMPRSS2 Fluorogenic Substrate (5 mM) | 10 µl | -20°C (Protect from light) |
78048 | 1x TMPRSS2 Assay Buffer | 5 ml | -20°C |
78049 | Camostat | 500 µg | -80°C |
79685 | 96-well black plate | 1 | Room Temp |
*The concentration of the protein is lot-specific and will be indicated on the tube
TMPRSS2 is a serine protease that facilitates SARS-CoV-2 particle entry into host cells via priming of the viral protein Spike. Its inhibition blocks the fusion of the virus with the plasma membrane after Spike interacts with human receptor Angiotensin-converting enzyme 2 (ACE2), restricting SARS-CoV-2 viral entry, therefore TMPRSS2 is an important therapeutic target for the treatment of COVID-19.
The protein may also play a role in prostate cancer because its gene is frequently altered in tumor cells. Indeed, TMPRSS2-ERG and TMPRSS2-ETV1 fusions are frequent, with TMPRSS2-ERG present in approximately 40 to 80% of human prostate tumors. ETS-related gene (ERG) is a transcription factor that regulates the expression of genes involved in embryonic development, cell proliferation and differentiation, and apoptosis, acting as an oncogene. Alternatively, the tumor suppressor function of TMRSS2 is disrupted since the fusion genes arise from deletions that eliminate the TMPRSS2 coding region while juxtaposing its androgen-inducible promoter and the open reading frame of ERG. Overexpression of ERG contributes to development of androgen-independence in prostate cancer through disruption of androgen receptor signaling.
1. Tomlins, S. A., et al.,2008. "Role of the TMPRSS2-ERG gene fusion in prostate cancer." Neoplasia 10(2): 177-IN9.
2. Hoffmann, M., et al., 2020. “SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor”. Cell 181: 271–280.