Ki: 1 μM (Keap1)

ML334 (LH601A; 50-100 µM; 6-16 hours; HEK293 cells) treatment increases NQO1 and TRX1 mRNAs between 2- and 3-fold at both 6 and 16 h. And also enhances HO-1 mRNA expression between 4- and 7-fold at 6 h, with lesser fold-changes at 16 h. ML334 (LH601A; 50-100 µM; 16 hours; HEK293 cells) treatment induces HO-1 and TRX1 proteins in HEK293 cells. ML334 (LH601A) stimulates NRF2 expression and nuclear translocation in HEK293 cells. RT-PCR Cell Line: HEK293 cells Concentration: 50 μM or 100 µM Incubation Time: 6 hours, 16 hours Result: Increased NQO1 and TRX1 mRNAs between 2- and 3-fold at both 6 and 16 h. Enhanced HO-1 mRNA expression between 4- and 7-fold at 6 h. Western Blot Analysis Cell Line: HEK293 cells Concentration: 50 μM or 100 µM Incubation Time: 16 hours Result: Enhanced HO-1 and TRX1 protein expression at 16 h.

ML334 (LH601A) 是一种有效的，细胞可渗透的 NRF2 激活剂，通过抑制 Keap1-NRF2 蛋白质相互作用来发挥作用。ML334 以 Kd 值为 1μM 来结合 Keap1 Kelch 域。ML334 刺激 NRF2 表达和核易位并诱导抗氧化反应元件 (ARE) 活性。