CAY10682

A dual inhibitor of p53-Mdm2 interaction and NF-κB signaling

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库存: 现货

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1mg

￥1962.00

1570.00

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5mg

￥8787.00

7030.00

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10mg

￥15437.00

12350.00

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货号: ajci70622
CAS: 1542066-74-9
别名:
分子式: C30H25BrFN5O
分子量: 570.5
纯度: >98%
溶解度: DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml,Ethanol: 2 mg/ml
储存: Store at -20°C
库存: 现货

Background

(±)-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.