nrf2in4

4-(5-Bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-amine is a brominated pyrrolopyridine-based scaffold designed for advanced medicinal chemistry and kinase inhibitor development. Its 7-azaindole (pyrrolopyridine) core serves as a purine bioisostere capable of occupying ATP-binding pockets across diverse kinases. The bromine substituent at the 5-position offers both electronic tuning and a versatile handle for cross-coupling reactions, enabling rapid SAR exploration. The 2-aminopyrimidine moiety further supports hinge-binding interactions, collectively making 4-(5-Bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-amine a valuable starting point for generating FGFR-targeted inhibitors and other kinase-directed therapeutics.

Nrf2-IN-4 is an Nrf2 inhibitor that induces ferroptosis by disrupting cellular iron homeostasis, promoting ferritin degradation, and ultimately triggering ferroptosis. It activates lysosomes through iron-dependent reactive oxygen species (ROS) production and lysosomal acidification. Nrf2-IN-4 demonstrates significant antitumor effects and is applicable in breast cancer research.

Keap1-Nrf2-IN-4, a powerful neddylation inhibitor, demonstrates significant anti-proliferation activity against MGC-803 cells (IC50 = 2.55 μM), effectively impeding their migration and inducing apoptosis. Additionally, it effectively inhibits tumor growth while exhibiting minimal toxicity [1].