TMPRSS2 Fluorogenic Assay Kit1

• Background:

  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.

• Description:

  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 ourProtease Screening ServicesorCoronavirus Services.This product has beencited 11 times.

• UniProt:

  O15393

• Applications:

  Study enzyme kinetics and screen small molecular inhibitors in high throughput (HTS) applications

• Format:

  Catalog #NameAmountStorageTMPRSS2*15 µg-80°C78047TMPRSS2 Fluorogenic Substrate (5 mM) 10 µl-20°C (Protect from light) 780481x TMPRSS2 Assay Buffer5 ml-20°C78049Camostat500 µg-80°C7968596-well black plate1Room Temp*The concentration of the protein is lot-specific and will be indicated on the tube

• Shipping Conditions:

  -80°C

• Storage Conditions:

  This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.

• Notes:

  Troubleshooting GuideVisitbpsbioscience.com/assay-kits-faqfor detailed troubleshooting instructions. For all further questions, please email[email protected]

• Contraindications:

  The final concentration of DMSO in the assay should not exceed . Higher DMSO concentrations can significantly decrease the activity of the enzyme.