degrasyn

Degrasyn, also known as WP1130, is a small molecule, second-generation tyrphostin derivative that functions as a cell-permeable, selective deubiquitinase (DUB) inhibitor. It targets several deubiquitinating enzymes, including USP9x, USP5, USP14, UCH37 (UCHL5), and UCH-L1. By inhibiting these enzymes, degrasyn triggers the accumulation of polyubiquitinated proteins, which leads to the downregulation of key survival and signaling proteins such as Bcr-Abl, JAK2, and MCL-1, and the subsequent inhibition of the JAK-STAT signaling pathway. Preclinical research has explored its potential therapeutic applications in various malignancies, including chronic myelogenous leukemia (CML), mantle cell lymphoma, multiple myeloma, melanoma, glioblastoma, and pancreatic ductal adenocarcinoma. Additionally, degrasyn has demonstrated antimicrobial activity against multi-resistant Staphylococcus aureus. It is currently utilized primarily as a research tool compound and has not yet entered formal clinical development.

Other names

CAS 856243-80-6CAS856243-80-6CAS-856243-80-6