Inhibits the deubiquitinase activity of USP9x

WP1130 – 25 mg

Brand:
Cayman
CAS:
856243-80-6
Storage:
-20
UN-No:
Non-Hazardous - /

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 μM, 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}  

 

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Description

Inhibits the deubiquitinase activity of USP9x, USP5, USP14, and UCH37; 5 μM induces the accumulation of protein-ubiquitin conjugates, resulting in the formation of aggresomes and apoptosis in a variety of tumor cells

Formal name: (2E)-3-(6-bromo-2-pyridinyl)-2-cyano-N-[1S-phenylbutyl]-2-propenamide

Synonyms:  Degrasyn

Molecular weight: 384.3

CAS: 856243-80-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Product Type|Biochemicals|Small Molecule Inhibitors|Ubiquitin Ligase System||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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