Products/Services Used | Details | Operation |
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Gene Synthesis | UCHL1, UCHL1C90A, and UCHL3 (Expressed in pET15b by GenScript) for biochemical assays were grown in LB growth medium at 37 °C to an optical density of 0.6–0.8. | Get A Quote |
The deubiquitinating enzyme (DUB) UCHL1 is implicated in various disease states including neurodegenerative disease and cancer. However, there is a lack of quality probe molecules to gain a better understanding on UCHL1 biology. To this end a study was carried out to fully characterize and optimize the irreversible covalent UCHL1 inhibitor VAEFMK. Structure-activity relationship studies identified modifications to improve activity versus the target and a full cellular characterization was carried out for the first time with this scaffold. The studies produced a new inhibitor, , with an IC value of 7.7 µM against UCHL1 and no observable activity versus the closest related DUB UCHL3. The molecule was also capabl... More