ML334  (Synonyms: LH601A)

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 K_d of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity^[1][2].

Ki: 1 μM (Keap1)^[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

446.50

Solid

C₂₆H₂₆N₂O₅

1432500-66-7

O=C(C1=CC=CC=C1C2=O)N2C[[email protected]@H]3C4=CC=CC=C4CCN3C([[email protected]]5[[email protected]](CCCC5)C(O)=O)=O

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

• [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.  [Content Brief]

  [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.  [Content Brief]