P22077 is a cell permeable inhibitor of the ubiquitin-specific protease USP7 (IC50=8.6 µM), and the closely related deubiquitinase (DUB) USP47. P22077 showed weak or no inhibition (EC50 >50µM) towards a panel of 14 isopeptidases and other proteases. Treatment of cells with P22077 (20–40 µM) causes an accumulation of K48-linked ubiquitinated species, and down regulation of the USP7 targets HDM2 and claspin.

Ethanone, 1–[5–[(2,4–difluorophenyl)thio]–4–nitro–2–thienyl]–

≥98% by HPLC.

Soluble in DMSO

Light powder

Store at +4°C. Stable as supplied for up to 2 years when stored dessicated at +4°C. Store solutions at -20°C for up to 1 month.

Useful for inhibition of USP7 and USP47 activity.

1. Altun, M., et al. , Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem Biol, 2011. 18(11): p. 1401-12.
2. Tian, X., et al., Characterization of selective ubiquitin and ubiquitin-like protease inhibitors using a fluorescence-based multiplex assay format. Assay Drug Dev Technol, 2011. 9(2): p. 165-73.

Protect from moisture.

Protease

Inhibitors/Activators