Nrf2 activator-6, a tetrahydroisoquinoline compound, is a Nrf2 activator. Nrf2 activator-6 has an IC50 of 5 nM for inhibiting the Kelch domain-Nrf2 interaction (WO2021214470A1; Example 4)[1].
NRF2 inhibitor AEM1 is a specific small molecule inhibitor of Nrf2 transcriptional activity in cancer cells, shows no activity against a panel of >100 kinases (including isoforms of PI3K, AKT, and PKC); broadly decreases the expression of Nrf2 controlled genes (HMOX1, GPX2), sensitizes A549 cells to various chemotherapeutic agents, and inhibits the growth of A549 cells in vitro and in vivo.
Bardoxolone is a novel nuclear regulator factor (Nrf-2) activator.
CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator.
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