ML334 (Synonyms: LH601) |
| カタログ番号GC38819 |
ML334 は、Keap1-NRF2 タンパク質間相互作用の阻害による NRF2 の強力な細胞透過性活性化因子です。 ML334 は 1 μM の Kd で Keap1 Kelch ドメインに結合します。 ML334 は、NRF2 の発現と核移行を刺激し、抗酸化応答要素 (ARE) 活性を誘導します。
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Cas No.: 1432500-66-7
Sample solution is provided at 25 µL, 10mM.
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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.
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