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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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CSN5i-3 化学構造

Cas No.: 2375740-98-8

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$1,010.00
在庫あり
1mg
$380.00
在庫あり
5mg
$908.00
在庫あり
10mg
$1,391.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

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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