Merck, 5059870001, Keap1-Nrf2 Interaction Probe, ML334

General description
A cell-permeable tetrahydroisoquinoline derivative that acts as a direct, non-covalent inhibitor of Keap1 - Nrf2 (Kelch-like ECH-associated protein 1 - nuclear factor erythroid 2-related factor 2) protein - protein interaction (Kd = 1 µM) that causes the dissociation of Nrf2 from keap1 in the cytosol. Exhibits ARE-inducing activity (EC₅₀ = 18 µM in U2OS Keap1-Nrf2 functional assay) and promotes Nrf2 translocation to the nucleus (EC₅₀ = 12 µM). Has good solubility in aqueous buffers (>100 µM in phosphate buffered saline).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Primary Target
Keap1–Nrf2
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Hu, L., et al, 2013, Bioorg. Med. Chem. Lett.23, 3039.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)