(±)-Nutlin-3 (Item No. 10004372) 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.¹ CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (K_i = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway.² It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKKɛ (IC₅₀s = 80.5, 78.2, and 57.1 µM, respectively).² 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.²

≥98%

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1.Vassilev, L.T.,Vu, B.T.,Graves, B., et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science 303, 844-848 (2004).

2.Zhuang, C.,Miao, Z.,Wu, Y., et al. Double-edged swords as cancer therapeutics: Novel, orally active, small molecules simultaneously inhibit p53-MDM2 interaction and the NF-κB pathway. Journal of Medicinal Chemistry 57(3), 567-577 (2014).