Biochem/physiol Actions
Reversible: yes
Primary TargetKeap1–Nrf2
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).
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Hu, L., et al, 2013, Bioorg. Med. Chem. Lett.23, 3039.
Packaging
Packaged under inert gas
10 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Warning
Toxicity: Standard Handling (A)
This product has met the following criteria: