Keap1-Nrf2 Interaction Probe, ML334

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 (K_d = 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).

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 (K_d = 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.

Primary Target
Keap1–Nrf2

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Hu, L., et al, 2013, Bioorg. Med. Chem. Lett.23, 3039.

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