114480-06-7

Upstream product

• 2389-48-2 N-ε-tert-butoxycarbonyl-L-lysine methyl ester hydrochloride 
• 114480-07-8 (S)-2-((S)-2-(((benzyloxy)carbonyl)amino)-3-phenylpropanamido)-6-((tert-butoxycarbonyl)amino)hexanoic acid 
• 2418-95-3 (S)-2-amino-6-(tert-butoxycarbonylamino)hexanoic acid 
• 769922-77-2 (S)-benzyl (1-(1H-benzo[d][1,2,3]triazol-1-yl)-1-oxo-3-phenylpropan-2-yl)carbamate 
• 42362-08-3 (S)-methyl 2-((S)-2-(((benzyloxy)carbonyl)amino)-3-phenylpropanamido)-6-((tert-butoxycarbonyl)amino)hexanoate 
• 186581-53-3 diazomethane 
• 114480-08-9 C₂₉H₃₇N₅O₆ 

Downstream Products

• 1252585-62-8 Z-Phe-Lys-CH₂-Br 
• 1252585-71-9 C₃₈H₄₁F₆N₃O₈ 
• 1252585-70-8 Z-Phe-Lys(Boc)-methyl (4-methyl)benzoate 
• 1252585-72-0 C₃₇H₄₅N₃O₉ 
• 1252585-69-5 C₃₆H₄₃N₃O₈ 
• 1252585-73-1 Z-Phe-Lys(Boc)-methyl (4-nitro)benzoate 

Relevant academic research and scientific papers

Increasing time on target: utilization of inhibitors of cysteine cathepsins to enhance the tumor retention of receptor-targeted agents

We report a strategy of utilizing irreversible cysteine cathepsin inhibitor as trapping agent to increase the tumor residence time of receptor-targeted agents. The targeted constructs incorporating these cysteine cathepsin trapping agents were able to for

RADIOPHARMACEUTICALS AND METHODS OF USE THEREOF

Targeted pharmaceuticals, particularly targeted radiopharmaceuticals, are provided which possess extended tumor retention time.

PHOTODYNAMIC QUENCHED ACTIVITY BASED PROBES AND USES THEREOF IN IMAGING AND TARGETED THERAPY

The present invention relates to compounds comprising photosensitizer, compositions comprising the same as well as uses and methods thereof for detection and for treatment using photodynamic therapy.

Synthesis and evaluation of radioiodinated acyloxymethyl ketones as activity-based probes for cathepsin B

Dipeptidyl (acyloxy)methyl ketones (AOMKs) were functionalized with different iodine-containing prosthetic groups to generate a library of candidate cathepsin B probes. Compound 23a, (S)-20-[(S)-2-{[(benzyloxy)carbonyl]amino}-3-phenylpropanamido]-1-(4-iod

Modulation of the inhibitor properties of dipeptidyl (acyloxy)methyl ketones toward the CaaX proteases

Dipeptidyl (acyloxy)methyl ketones (AOMKs) have been identified as mechanism-based inhibitors of certain cysteine proteases. These compounds are also inhibitors of the integral membrane proteins Rce1p and Ste24p, which are proteases that independently mediate a cleavage step associated with the maturation of certain isoprenylated proteins. The enzymatic mechanism of Rce1p is ill-defined, whereas Ste24p is a zinc metalloprotease. Rce1p is required for the proper processing of the oncoprotein Ras and is viewed as a potential target for cancer therapy. In this study, we synthesized a small library of dipeptidyl AOMKs to investigate the structural elements that contribute to the inhibitor properties of this class of molecules toward Rce1p and Ste24p. The compounds were evaluated using a fluorescence-based in vitro proteolysis assay. The most potent dipeptidyl AOMKs contained an arginine residue and the identity of the benzoate group strongly influenced potency. A 'warhead' free AOMK inhibited Rce1p and Ste24p. The data suggest that the dipeptidyl AOMKs are not mechanism-based inhibitors of Rce1p and Ste24p and corroborate the hypothesis that Rce1p is not a cysteine protease.