ML385是一种新型选择性Nrf2抑制剂，IC50为1.9 μM。

ML385 is a new-type and selective NRF2 inhibitor.

ML385 reduce the NRF2 transcriptional activity in a dose-dependent manner with the maximum inhibitory concentration is 5 μM. ML385 interacts with NRF2 and affects the DNA binding activity of the NRF2-MAFG protein complex（IC50=1.9 μM）.

ML385 in combination with carboplatin leads to a significant reduction in tumor cell proliferation, demonstrated by fewer Ki-67 positive cells. Tumor samples treated with ML385 show a significant reduction in NRF2 protein level and its downstream target genes.

cells are treated with ML385 for 36 h. An equal amount of CellTiter-Blue reagent is added to the wells and the fluorescence is measured after 30 min. The CellTiter-Blue reagent is discarded and the Caspase-Glo (100 μL) reagent is added to the cells and incubated at 37°C for an additional 60-90 min. The resulting luminescence is recorded and the caspase activity is normalized to cell number

Mice tumor xenografts are administered intraperitoneally ML385 (30 mg/kg).

846557-71-9

C29H25N3O4S

511.6

DMSO:30 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years