CSN5i-3 |
カタログ番号GC34340 |
CSN5i-3は、CSN5/Jab1の強力で選択的な経口投与可能な阻害剤であり、IC50値が5.8nMであるCSN触媒によるCul1デネドリレーションを阻害します。
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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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