Nrf2-IN-3 (Compound R16) is a small-molecule NRF2 inhibitor and increases reactive oxygen species (ROS) production. Nrf2-IN-3 selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions, leading to proteasome-dependent NRF2 degradation in cells. Nrf2-IN-3 sensitizes KEAP1-mutated tumor cells to Cisplatin (HY-17394), Gefitinib (HY-50895), and KEAP1 G333C-mutated xenograft to Cisplatin [1].
Molekulargewicht:
442.53
Reinheit:
99.19
CAS Nummer:
[6325-13-9]
Formel:
C22H26N4O4S
Target-Kategorie:
Keap1-Nrf2,Reactive Oxygen Species (ROS)
Anwendungsbeschreibung:
Reference compound
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