In heterogeneous catalysis, the catalyst is in a different phase from the reactants. name: (S)-1,2,3,4-Tetrahydroisoquinoline-1-carboxylic acid, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 151004-92-1, name is (S)-1,2,3,4-Tetrahydroisoquinoline-1-carboxylic acid. In an article£¬Which mentioned a new discovery about 151004-92-1
Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction
A high-throughput screen (HTS) of the MLPCN library using a homogenous fluorescence polarization assay identified a small molecule as a first-in-class direct inhibitor of Keap1-Nrf2 protein-protein interaction. The HTS hit has three chiral centers; a combination of flash and chiral chromatographic separation demonstrated that Keap1-binding activity resides predominantly in one stereoisomer (SRS)-5 designated as ML334 (LH601A), which is at least 100¡Á more potent than the other stereoisomers. The stereochemistry of the four cis isomers was assigned using X-ray crystallography and confirmed using stereospecific synthesis. (SRS)-5 is functionally active in both an ARE gene reporter assay and an Nrf2 nuclear translocation assay. The stereospecific nature of binding between (SRS)-5 and Keap1 as well as the preliminary but tractable structure-activity relationships support its use as a lead for our ongoing optimization.
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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem