108456-25-3

Upstream product

• 51871-42-2 (S)-2-(2-(tert-butoxycarbonylamino)acetamido)-4-methylpentanoic acid 
• 7524-50-7 methyl (2S)-2-amino-3-phenylpropanoate hydrochloride 
• 4530-20-5 BOC-glycine 
• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 
• 13139-15-6 N-tert-butoxycarbonyl-L-leucine 
• 6461-07-0 methyl (S)-2-[(S)-2-amino-4-methylpentanamido]-3-phenylpropanoate hydrochloride 
• 15136-32-0 (N-(tert-butoxycarbonyl)-L-leucinyl)-L-phenylalanine methyl ester 
• 2577-90-4 methyl (2S)-2-amino-3-phenylpropanoate 

Downstream Products

• 1414357-91-7 methyl (S)-2-((S)-2-{2-[(S)-2-azidopropanamido]acetamido}-4-methylpentanamido)-3-phenylpropanoate 
• 1414357-46-2 methyl (S)-2-{(S)-2-[2-((S)-2-{4-[(8R,9S,13S,14S,17S)-3,17-dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6Hcyclopenta[a]phenanthren-17-yl]-1H-1,2,3-triazol-1-yl}propanamido)acetamido]-4-methylpentanamido}-3-phenylpropanoate 

Relevant academic research and scientific papers

Microwave-Assisted Synthesis of 2,2′-Azopyridine-Labeled Amines, Amino Acids, and Peptides

A microwave-assisted procedure for labeling amines, amino acids, and peptides with 2,2′-azopyridines (2,2′-AzPy) is described using the corresponding 2,2′-azopyridine-diacylbenzotriazoles. The efficiency of the procedure is proven by the generation of thr

Preparation and biological evaluation of soluble tetrapeptide epoxyketone proteasome inhibitors

A series of novel tetrapeptidyl epoxyketone inhibitors of 20S proteasome was designed and synthesized. To fully understand the SAR, various groups at R1, R2, R3, R4 and R5 positions, including aromatic and aliphatic substituents were designed, synthesized and biologically assayed. Based on the enzymatic results, seven compounds were selected to evaluate their cellular activities and soluble compound 36 showed strong potency against human multiple myeloma (MM) cell lines. Microsomal stability results indicated that compound 36 was more stable in mice, rat and human microsomes than marketed carfilzomib. The in vivo activities of this compound were evaluated with the xenograft mice models of MM cell lines ARH77 and RPMI-8226 with luciferase expression and the T/C value of the two models were 49.5% and 37.6%, respectively. To evaluate the potential cardiovascular toxicity, inhibition of hERG ion channel in HEK293 cells by compound 36 and carfilzomib was carried out. The results indicated that 36 had no binding affinity for the hERG ion channel while carfilzomib could bind it with IC50 of 92.1 μM.

17α-ethynylestradiol peptide labeling by 'click' chemistry

A synthesis of 17α-ethynylestradiol-labeled native peptides is reported. The peptide moiety is tethered to the steroid hormone by a 1,2,3-triazole bridge formed by a CuAAC reaction in which the azido group of the peptide combines with the terminal acetylenic moiety of ethynylestradiol to link the two bioactive molecules. Thus bioconjugates containing the hormone moiety at three positions within the peptide molecule could be useful targets for hormono-enzyme interaction studies. Georg Thieme Verlag Stuttgart ? New York.