Cayman Chemical ACE2 Inhibitor Screening Assay Kit

Cayman Chemical’s ACE2 Inhibitor Screening Assay Kit provides a robust and easy-to-use platform to identify potential inhibitors of human angiotensin-converting enzyme 2 (ACE2), with results in 30 min.

ACE2 has roles in regulating blood pressure, fluid homeostasis, cardiac contractility, amino acid absorption and the prevention of pulmonary fibrosis and hypertension. It also acts as the functional receptor for severe acute respiratory syndrome coronavirus (SARS-CoV) and SARS-CoV-2 to facilitate viral entry into host cells. Inhibitors of the ACE2 and SARS-CoV-2 interaction may play a role in preventing viral infection that leads to COVID-19. But given the important homeostatic functions of ACE2, inhibiting this enzyme can adversely affect blood pressure. Such inhibitors may bar viral fusion while dually increasing angiotensin II-induced hypertension, susceptibility to atherosclerotic plaques, myocardial dysfunction and insulin resistance, thereby exacerbating COVID-19 comorbidities.

The ACE2 Inhibitor Screening Assay Kit can be used as a toxicity screen of a wide range of drug candidates, including those that inhibit the ACE2/SARS-CoV-2 interaction, so that they do not interfere with the normal physiological functions of ACE2. To detect ACE2 activity, the assay uses an ACE2-specific fluorogenic substrate, Mca-APK (Dnp). ACE2 cleaves this substrate generating free Mca, which is quantified using a fluorescence plate reader. The addition of an effective inhibitor will suppress this fluorescence. The kits conveniently package the ACE2 enzyme, substrate and buffer, and include a potent ACE2 inhibitor (MLN-4760) as a positive control to ensure proper assay performance. The kit has a robust Z′ factor of 0.96.