CSN5i-3 |
| رقم الكتالوجGC34340 |
CSN5i-3 هو مثبط فعال وانتقائي ومتاح عن طريق الفم لـ CSN5 / Jab1 ، ويثبط تجلط Cul1 المحفز بواسطة CSN بقيمة IC50 تبلغ 5.8 نانومتر.
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.
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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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