PR-619,DeubiquitinylatingEnzyme(DUB)Inhibitor

PR-619 is a cell-permeable, non-selective, reversible broad-range inhibitor of the deubiquitinylating enzymes (DUBs) with IC₅₀ of 1-20 μM. PR-619 is shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150 μM, 0.5 to 20 h) without direct impairment of proteasomal proteolysis. PR-619 treatment results in upregulation of both K⁴⁸ - and K⁶³-linked polyUb chains. It induces HCT116 cell death with EC₅₀ ~6.3 μM.

How to Use:

• In vitro: PR-619 was used at 10-50 µM final concentration in various in vitro assays.
• In vivo: n/a

Reference:

1. 1. Altun M, et al. Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. (2011) Chem Biol. 18(11):1401-12.

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