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ML334
- LH601A
Axon 2641
CAS:
1432500-66-7
Purity:
99%
- Soluble in DMSO
- MF: C26H26N2O5
- MW: 446.5
Description
Activator of NRF2 signaling by inhibition of Keap1-NRF2 protein-protein interaction (PPI; IC50 value 1.6 - 2.3 µM in a fluorescence polarisation assay using Keap1 Kelch domain/NRF2-ETGE peptide; Kd value 1 μM to Keap1 Kelch domain). ML 334 stimulates NRF2 expression and nuclear translocation, and induces antioxidant response elements (ARE) and transcription of HO-1 and TRX1 proteins.
More Information
| Parent CAS No. | 1432500-66-7 |
|---|---|
| Chemical Name | (1S,2R)-2-((S)-1-((1,3-dioxoisoindolin-2-yl)methyl)-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)cyclohexanecarboxylic acid |
| MFCD | N.A. |
| Short Description | NRF2 acitivator |
References
- L Hu 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.
- X Wen 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.
- E Jnoff et al. Binding mode and structure-activity relationships around direct inhibitors of the Nrf2-Keap1 complex. ChemMedChem. 2014 Apr;9(4):699-705.
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