MG-115 is a peptidyl aldehyde analog combining hydrophobic and aromatic residues with a reactive terminal group. The structure supports studies of protease engagement, conformational transitions, and covalent-binding mechanisms. Researchers employ it in kinetic profiling and structural evaluation. Its functional flexibility aids mechanistic exploration.
CAT No: R2192
CAS No:133407-86-0
Synonyms/Alias:MG-115;Z-LL-Nva-CHO;133407-86-0;MG115;benzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxopentan-2-yl]amino]pentan-2-yl]amino]-1-oxopentan-2-yl]carbamate;DTXSID00432100;n-benzyloxycarbonyl-l-leucyl-l-leucyl-l-norvalinal;Cbz-Leu-Leu-norvalinal;Carbobenzoxy-L-leucyl-L-leucyl-L-norvalinal;benzyl N-((2S)-4-methyl-1-(((2S)-4-methyl-1-oxo-1-(((2S)-1-oxopentan-2-yl)amino)pentan-2-yl)amino)-1-oxopentan-2-yl)carbamate;carbobenzoxy-leucyl-leucyl-norvalinal;Curator_000004;SCHEMBL2140161;CHEMBL4518490;CHEBI:95100;EX-A1500B;GTPL11639;DTXCID50382929;QEJRGURBLQWEOU-FKBYEOEOSA-N;BDBM476985;AKOS040744889;NCGC00345815-01;DA-55451;HY-108552;CS-0029136;G12577;Z-Leu-Leu-Norvalinal, >=90% (HPLC), powder;Q27166869;N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxopentan-2-yl]amino]pentan-2-yl]amino]-1-oxopentan-2-yl]carbamic acid (phenylmethyl) ester;
MG-115 is a synthetic peptide aldehyde widely recognized as a potent, cell-permeable proteasome inhibitor. As a tripeptide derivative, it specifically targets and inhibits the chymotrypsin-like and, to a lesser extent, the trypsin-like activities of the 20S proteasome complex. By blocking proteasomal degradation, MG-115 disrupts the ubiquitin-proteasome pathway, a central cellular mechanism for regulated protein turnover. Its high specificity and reversible inhibitory action make it a valuable research tool for dissecting the roles of proteasomal activity in various cellular and molecular processes, particularly those involving protein quality control, signal transduction, and apoptosis.
Proteasome inhibition: MG-115 is extensively used in studies of proteasome function due to its ability to selectively and reversibly block proteolytic activity within the 20S core particle. Researchers employ this compound to investigate the consequences of impaired protein degradation, enabling detailed analysis of the accumulation of ubiquitinated substrates and the downstream effects on cellular homeostasis. Its application has been instrumental in elucidating the molecular underpinnings of protein turnover and the maintenance of proteostasis in both normal and stressed cellular environments.
Cell signaling research: The compound is a powerful tool for exploring the regulatory influence of the ubiquitin-proteasome system on key signaling pathways. By inhibiting proteasome-mediated degradation of specific signaling proteins, MG-115 allows for the stabilization and accumulation of transcription factors, cell cycle regulators, and other labile proteins. This facilitates the study of signal transduction cascades, such as those involving NF-κB, where proteasomal processing is essential for activation or repression. Such research provides critical insight into the dynamic modulation of cellular responses under various physiological and experimental conditions.
Apoptosis and cell death studies: MG-115 is frequently utilized to probe the relationship between proteasome inhibition and programmed cell death. By preventing the degradation of pro-apoptotic and anti-apoptotic factors, it enables researchers to dissect the molecular events that govern apoptosis initiation, execution, and regulation. Use of this inhibitor has advanced understanding of the interplay between proteasomal activity, caspase activation, and mitochondrial integrity, offering a mechanistic basis for investigating cellular stress responses and survival pathways in diverse model systems.
Protein quality control investigations: The peptide aldehyde is valuable for characterizing the cellular machinery involved in protein quality surveillance. By interfering with the removal of misfolded, damaged, or regulatory proteins, MG-115 creates a controlled environment for studying the consequences of proteostasis disruption. Researchers leverage its effects to model pathological states associated with impaired protein degradation, such as neurodegenerative disease mechanisms or aggregation-prone protein disorders, thereby gaining insights into cellular strategies for managing proteotoxic stress.
Biochemical assay development: MG-115 serves as a reference inhibitor in the development and validation of in vitro proteasome activity assays. Its well-defined inhibitory kinetics and specificity make it an ideal positive control for benchmarking assay sensitivity and selectivity. In addition, it is used to standardize experimental conditions in studies requiring precise modulation of proteasomal function, supporting robust and reproducible biochemical analyses in both academic and industrial research settings.
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