CAY10682

(±)-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

WARNING This product is not for human or veterinary use.

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(5659), 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. J. Med. Chem. 57(3), 567-577 (2014).