1123546-32-6

Upstream product

• 1123546-42-8 2-[3-(N'-tert-butoxycarbonylhydrazino)-4,4,4-trifluorobutyrylamino]-3-phenyl-propionic acid methyl ester 
• 76-05-1 trifluoroacetic acid 

Downstream Products

• 1123546-15-5 2-{3-[N'-(6-benzyloxycarbonylamino-2-tert-butoxycarbonylaminohexanoyl)hydrazino]-4,4,4-trifluorobutyrylamino}-3-phenylpropionic acid methyl ester 
• 1123546-35-9 2-(3-{N'-[3-(3,4-dimethoxyphenyl)-2-(9H-fluoren-9-ylmethoxycarbonylamino)propionyl]hydrazino}-4,4,4-trifluorobutyrylamino)-3-phenylpropionic acid methyl ester 

Relevant academic research and scientific papers

α- and β-hydrazino acid-based pseudopeptides inhibit the chymotrypsin-like activity of the eukaryotic 20S proteasome

We describe the synthesis of a library of new pseudopeptides and their inhibitory activity of the rabbit 20S proteasome chymotrypsin-like (ChT-L) activity. We replaced a natural α-amino acid by an α- or a β-hydrazino acid and obtained inhibitors of proteasome up to a submicromolar range (0.7 μM for molecule 24b). Structural variations influenced the inhibition of the ChT-L activity. Models of inhibitor/20S proteasome complexes corroborated the inhibition efficacies obtained by kinetic studies.

Novel fluorinated pseudopeptides as proteasome inhibitors

We have designed novel small inhibitors of rabbit 20S proteasome using a trifluoromethyl-β-hydrazino acid scaffold. Structural variations influenced their inhibition of the three types of active sites. Proteasome inhibition at the micromolar level was sel