tcsc1513 PR-619

PR-619 is a broad-range DUB inhibitor with EC₅₀ of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively.

IC50 & Target: EC50: 3.93 μM (USP4), 4.9 μM (USP8), 6.86 μM (USP7), 7.2 μM (USP2), 8.61 μM (USP5)^[1]

In Vitro: PR-619, a deubiquitylase inhibitor, prevents degradation, indicating KCa3.1 is targeted for degradation by ubiquitylation. In PR-619 treated cells, channel degradation is significantly inhibited with 87±1% of KCa3.1 still remaining after 24 hrs (n=3; P<0.05)^[2]. Cell viability is determined by MTT assay and revealed that PR-619 exerted concentration-dependent cytotoxicity in a very narrow concentration range of 7-10 μM^[3].