Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling.¹ It potently binds MDM2 (K_i = 250 nM), reducing MDM2-mediated turnover of p53.¹ CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65.¹ It blocks the proliferation of cancer cell lines (IC₅₀s range from 33 to 37 µM).¹ CAY10681 exhibits excellent oral bioavailability and inhibits tumor growth in A549 xenografts in nude mice.¹

≥98%

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1.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).