CSN5i-3 |
Catalog No.GC34340 |
CSN5i-3 es un inhibidor potente, selectivo y disponible por vía oral de CSN5/Jab1, e inhibe la desnedilación de Cul1 catalizada por CSN con un valor IC50 de 5.8 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2375740-98-8
Sample solution is provided at 25 µL, 10mM.
CSN5i-3 is a potent, selective and orally available inhibitor of CSN5; inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8 nM.
CSN5i-3 traps CRLs in the neddylated state, which leads to inactivation of a subset of CRLs by inducing degradation of their substrate recognition module[1].
CSN5i-3 shows a good pharmacokinetic profile. CSN5i-3 inhibits growth of human xenograft. Treatment with CSN5i-3 triggers the formation of cleaved PARP and cleaved caspase 3 indicative of apoptosis induction[1].
[1]. Schlierf A, et al. Targeted inhibition of the COP9 signalosome for treatment of cancer. Nat Commun. 2016 Oct 24;7:13166.
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