WP1130

Territorial Availability: Available through Bertin Technologies only in France

• Synonyms
  • (2E)-3-(6-bromo-2-pyridinyl)-2-cyano-N-[1S-phenylbutyl]-2-propenamide
• Correlated keywords
  • Bcr/Abl anticancers Bcr Abl degrasyn deubiquintinase inhibitors inhibits inhibitions anti-tumors anti tumors antitumor bortezomib therapy therapies ubiquitin specific ubiquitin-specific protease apoptosis MCL-1 p53 MCL1 MCl 1 one WPs WP-1130 1130 tyrphostin derivatives deubiquitinating tumors proteins ubiquitination enzymes DUBs degradation proteasomes USPs UCHs COOH-terminal COOH terminal hydrolases activated cells transformed phenotypes WP1130 second-generation second generations USP9x 9x 9 x USP5 5 USP14 14 UCH37 37 tumor-activated induces accumulations protein-ubiquitin conjugates formations aggresomes mechanisms downregulates downs regulates down-regulate antiapoptotic Jak2 Jak 2 upregulates up up-regulate proapoptotic pro p 53
• Product Overview:
  Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into two subgroups: ubiquitin-specific proteases (USPs) and ubiquitin-specific COOH-terminal hydrolases (UCHs). Recent evidence suggests that several DUBs are activated in tumor cells and many contribute to a transformed phenotype.{24477} WP1130 is a second-generation tyrphostin derivative that inhibits the deubiquitinase activity of USP9x, USP5, USP14, and UCH37.{24478,24477} At 5 ?M, WP1130-mediated inhibition of tumor-activated DUBs induces a rapid accumulation of protein-ubiquitin conjugates, resulting in the formation of aggresomes and apoptosis in a variety of tumor cells.{24477} Through this mechanism, WP1130 has been shown to downregulate the antiapoptotic proteins Bcr/Abl and Jak2 and to upregulate the proapoptotic proteins MCL-1 and p53.{24477}