Catalog No.: PC-61193Not For Human Use, Lab Use Only.
CSN5i-3 (CSN5 inhibitor 3) is a potent, selective and orally available inhibitor of CSN5 with IC50 of 5.8 nM, the proteolytic subunit of COP9 signalosome (CSN).
CSN5i-3 (CSN5 inhibitor 3) is a potent, selective and orally available inhibitor of CSN5 with IC50 of 5.8 nM, the proteolytic subunit of COP9 signalosome (CSN).
CSN5i-3 displays >1,000-fold selectivity over JAMM domain proteases (Rpn11 and AMSHLP) and other metalloproteinases.
CSN5i-3 inhibits CSN-catalysed Cul1 deneddylation with IC50 of 5.8 nM, traps the cullin-RING E3 ubiquitin ligases (CRLs) in the neddylated state, and results in the inactivation of a subset of CRLs and the stabilization of their substrates.
CSN5i-3 exhibits a differentiating effect on the viability of cancer cells, inhibits growth of a human xenograft in vivo.
