RA839

RA839 is an inhibitor of the protein-protein interaction between Kelch-like ECH-associated protein 1 (Keap1) and nuclear factor erythroid 2-related factor 2 (Nrf2). It binds non-covalently to the Keap1 Kelch domain (Kd = ~6 µM). RA839 increases Nrf2-dependent transcription driven by antioxidant response element (ARE) in a reporter assay using HepG2 cells and induces Nrf2 nuclear translocation in U2OS cells (EC50 = 1.2 µM). It reduces LPS-induced increases in nitric oxide (NO) in bone marrow-derived macrophages (BMDMs) when used at concentrations ranging from 5 to 20 µM. RA839 (20 µM) reduces the levels of rotavirus structural proteins in infected MA-104 cells, an effect that is partially blocked by Nrf2 shRNA.2 It also decreases propagation of the rotavirus strains SA11, Wa, and A5-13 in MA-104 cells (IC50s = 10.303, 6.187, and 11.97 µM, respectively) and reduces viral titers in infected HT-29 and HEK293 cells (IC50s = 11.815 and 9.686 µM, respectively).. SMILES: CC1=C(C=C(C(C)=C1S(=O)(NC2=CC=C(C3=C2C=CC=C3)N4CC[C@H](C(O)=O)C4)=O)C)C. InChi Code: InChI=1S/C25H28N2O4S/c1-15-13-16(2)18(4)24(17(15)3)32(30,31)26-22-9-10-23(21-8-6-5-7-20(21)22)27-12-11-19(14-27)25(28)29/h5-10,13,19,26H,11-12,14H2,1-4H3,(H,28,29)/t19-/m0/s1. InChi Key: BVYWIQHJXAEJOD-IBGZPJMESA-N