Glycine, N,N'-1,4-naphthalenediylbis[N-[(4-methoxyphenyl)sulfonyl]-

CPUY192018 Disodium is a potent small-molecule inhibitor of the Keap1-Nrf2 PPI. CPUY192018 Disodium has a cytoprotective effect against DSS in both NCM460 cells and mouse colon via the activation of Nrf2 signaling. Activation of Nrf2 by directly inhibiting the Keap1-Nrf2 PPI may be beneficial as a treatment for ulcerative colitis.

CPUY192018 is a potent Keap1-Nrf2-ARE inhibitor with an IC50 of 0.63 μM. CPUY192018 exhibits induction of Nrf2-dependent gene NQO1 at 100 μM[1].

[1] Lee S, et al. Structure-activity relationships of 1,4-bis(arylsulfonamido)-benzene or naphthalene-N,N'-diacetic acids with varying C2-substituents as inhibitors of Keap1-Nrf2 protein-protein interaction. Eur J Med Chem. 2022; 237:114380. DOI:10.1016/j.ejmech.2022.114380