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CAY10682

カタログ番号GC43190

(±)-Nutlin-3は、p53とその負の調節因子であるMdm2の相互作用をブロックします(IC50 = 90 nM)、p53によって調節された遺伝子の発現を誘導し、in vivoで腫瘍キシェンクラフトの成長を阻害します。

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CAY10682 化学構造

Cas No.: 1542066-74-9

サイズ 価格 在庫数 個数
1mg
$163.00
在庫あり
5mg
$733.00
在庫あり
10mg
$1,302.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

(±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo. CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway. It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKK? (IC50s = 80.5, 78.2, and 57.1 µM, respectively). CAY10682 blocks the growth of cancer cells in vitro (IC50s = 2-6 µM) and inhibits the growth of A549 cell xenografts in mice without significantly reducing body weight.

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Average Rating: 5 ★★★★★ (Based on Reviews and 28 reference(s) in Google Scholar.)

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