Description
PR-619 (2645-32-1) is a nonselective, reversible inhibitor of cysteine-reactive deubiquitinating enzymes (DUBs; 5-20 μM)1. PR-619 is highly useful for preserving ubiquitinated proteins during cell lysis. DUBs become unregulated in cell lysates and will act quickly to deubiquitinate proteins of interest during cell lysis. To preserve maximum amounts of ubiquitinated protein, include PR-619 (50-100 μM) in lysis buffers. PR-619 is also useful for interrogating the role of DUBs in intact cell systems2, and treatment of cells results in an overall accumulation of ubiquitinated proteins and many other phenotypes.
Uses
PR-619 has been used:
- as a component of lysis buffer and also as a deubiquitinase inhibitor to treat proteins derived from SILAC-labeled Jurkat cells
- as a pan-deubiquitinase inhibitor to study its effect on adenoassociated virus (AAV) transduction
- in radioimmunoprecipitation assay buffer (RIPA) buffer used for ubiquitination assays
Uses
PR 619 is a broad-range DUB inhibitor. A selective and general inhibitior of cellular DUB activity without direct impairment of proteasomal proteolysis. Used in the preparation of thiazolopyridines an
d bisthiazolopyridines.
Biochem/physiol Actions
PR-619 is a cell permeable broad spectrum deubiquitylating enzymes (DBUs) inhibitor. PR-619 induces the accumulation of polyubiquitylated proteins in cells without directly affecting proteasome activity.
References
1) Altun?et al. (2011),?Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes; Chem. Biol.,?18?1401
2) Seiberlich?et al. (2012),?The small molecule inhibitor PR-619 of deubiquitinating enzymes affects the microtubule network and causes protein aggregate formation in neural cells: implications for neurodegenerative diseases; Biochim. Biophys. Acta,?1823?2057
