ML334 是一种有效的细胞渗透性 NRF2 激活剂，通过抑制 Keap1-NRF2 蛋白质-蛋白质相互作用。 ML334 与 Keap1 Kelch 结构域结合，Kd 为 1 μM。 ML334 刺激 NRF2 表达和核转位并诱导抗氧化反应元件 (ARE) 活性。
货号:ajcx15422
CAS:1432500-66-7
分子式:C26H26N2O5
分子量：446.5
溶解度:DMSO: 44.65 mg/mL (100.00 mM); Ethanol: 44.65 mg/mL (100.00 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity[1][2].

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[1].ML334 (LH601A; 50-100 µM; 16 hours; HEK293 cells) treatment induces HO-1 and TRX1 proteins in HEK293 cells[1].ML334 (LH601A) stimulates NRF2 expression and nuclear translocation in HEK293 cells[1]. RT-PCR[1] Cell Line: HEK293 cells

[1]. Wen X, et al. Activation of NRF2 Signaling in HEK293 Cells by a First-in-Class Direct KEAP1-NRF2 Inhibitor. J Biochem Mol Toxicol. 2015 Jun;29(6):261-6. [2]. Hu L, et al. Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. Bioorg Med Chem Lett. 2013 May 15;23(10):3039-43.