HOIPIN-8

HOIPIN-8 (HOIP inhibitor-8) is a potent, small-molecule inhibitor of the linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. It specifically targets the HOIP (RNF31) subunit of LUBAC, covalently binding to the active site Cys885 via Michael addition to inhibit its RING-HECT-hybrid E3 ubiquitin ligase activity. By blocking LUBAC-mediated Met1-linked linear ubiquitination, HOIPIN-8 suppresses the activation of the canonical NF-κB pathway and downstream inflammatory and antiviral signaling. Developed by Japan Tobacco and Osaka City University, HOIPIN-8 is widely utilized as a chemical probe in preclinical research to investigate linear ubiquitination pathways, inflammation, and potential therapeutic applications in cancer, psoriasis, and neurodegenerative diseases like amyotrophic lateral sclerosis (ALS).

Other names

HOIP inhibitor 8HOIP inhibitor-8HOIPIN8HOIPIN-8HOIPIN 8