ML334 (Synonyms: LH601) |
| Catalog No.GC38819 |
ML334 is a potent, cell-permeable activator of NRF2.
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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. It achieved through the inhibition of the Keap1-NRF2 protein-protein interaction. It demonstrates a binding affinity to Keap1 with a dissociation constant (Kd) of 1 μM in competitive surface plasmon resonance (SPR) assays. Furthermore, ML334 competes with an Nrf2 peptide, exhibiting an IC50 of 1.6 μM in fluorescence polarization (FP) assays[1-3].
ML334(100 μM; 3 hours) induces the expression and nuclear translocation of nuclear factor (erythroid-derived 2)-like 2 (NRF2) in HEK293 cells. Meanwhile, ML334 treatment induced the expression of HO-1 and TRX1 proteins in HEK293 cells [4].ML334-induced (50 μM; 48 hours) overexpression of Nrf2 enhances the antifibrotic effect of panaxatriol saponin (PTS) in cardiac fibroblasts[5].
[1]. Hu L, Magesh S, Chen L, Wang L, Lewis TA, Chen Y, Khodier C, Inoyama D, Beamer LJ, Emge TJ, Shen J, Kerrigan JE, Kong AN, Dandapani S, Palmer M, Schreiber SL, Munoz B. 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. doi: 10.1016/j.bmcl.2013.03.013. Epub 2013 Mar 14. PMID: 23562243; PMCID: PMC3648997.
[2]. Shen J, Magesh S, et,al. Enantiomeric characterization and structure elucidation of LH601A using vibrational circular dichroism spectroscopy. Spectrochim Acta A Mol Biomol Spectrosc. 2018 Mar 5;192:312-317. doi: 10.1016/j.saa.2017.11.033. Epub 2017 Nov 21. PMID: 29172127; PMCID: PMC10544735.
[3]. Wang L, Lewis T. et,al. The identification and characterization of non-reactive inhibitor of Keap1-Nrf2 interaction through HTS using a fluorescence polarization assay. 2012 Dec 17 [updated 2013 Sep 16]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. PMID: 24260785.
[4]. Wen X, Thorne G, 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. doi: 10.1002/jbt.21693. Epub 2015 Feb 12. PMID: 25683455; PMCID: PMC4713195.
[5]. Yao H, He Q, et,al. Panaxatriol saponin ameliorates myocardial infarction-induced cardiac fibrosis by targeting Keap1/Nrf2 to regulate oxidative stress and inhibit cardiac-fibroblast activation and proliferation. Free Radic Biol Med. 2022 Sep;190:264-275. doi: 10.1016/j.freeradbiomed.2022.08.016. Epub 2022 Aug 14. Erratum in: Free Radic Biol Med. 2023 Jun;202:34. PMID: 35977659.
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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