P-5091

Description

P5091 (882257-11-6) is a selective inhibitor of the ubiquitin-specific protease USP7 ( IC50=4.2 μM).1,2 Induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance.1?P5091 displays antiangiogenic activity in vivo.2?Cell permeable

The Uses of P-5091

P005091 is a selective dual inhibitor of the cancer-related deubiquitylating proteases USP7 and USP47.

The Uses of P-5091

P5091 has been used:

• as a ubiquitin specific peptidase 47 (USP47) inhibitor in 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay to evaluate the cellular viability of MCF-10A cells
• as a USP7 inhibitor to study the regulatory role for USP7 on inflammasome activation
• as USP7 inhibitor in drug susceptibility assays to study its effect on bone marrow?resident tumor cells (BMRTCs)/ circulating tumor cells (CTCs)

Biochem/physiol Actions

P5091 plays an important role in ovarian cancer, as it can prevent the growth of cells and can promote necrosis and apoptosis.

References

1) Chauhan et al. (2012), A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance; Cancer Cell, 22 345 2) Weinstock et al. (2012), Selective dual inhibitors of the cancer-related deubiquitylating proteases USP7 and USP47; ACS Med. Chem. Lett., 3 789