Figure 3: Inhibition profiles of 11 DUB inhibitors and inhibitor candidates.
From: Screening of DUB activity and specificity by MALDI-TOF mass spectrometry
Eleven different DUB inhibitors and inhibitor candidates were pre-incubated for 35 min at two different concentrations in duplicate (that is, two different experiments) with a panel of 32 DUBs and subsequently the specific substrate was added and incubated for 60 min (30 °C). Inhibition rates are colour coded with strongest inhibition in dark red, the diubiquitin topoisomers used for each DUB are in brackets. BAY 11-7082, NSC 697923 and SJB3-019A show some selectivity at 1 μM against USP7 and USP8, respectively, while PR-619 and HBX 41,108 inhibit strongly a wide range of DUBs even at low concentration. Other proposed inhibitors such as compound 16, L434078, WP1130 and P22077 show low activity and selectivity in this panel.
