Mca-PLGL-Dpa-AR-NH2 incorporates an Mca fluorophore and Dpa quencher flanking a protease-sensitive PLGL sequence. Cleavage separates donor and quencher, leading to fluorescence enhancement. Researchers employ the construct to quantify matrix metalloproteinase activity. Applications include real-time protease imaging in vitro, inhibitor screening, and kinetic-mechanism analysis.
CAT No: R2547
CAS No:1135689-33-6
Synonyms/Alias:Mca-PLGL-Dpa-AR-NH2;1135689-33-6;HY-P3474;DA-55275;PD076947;CS-0611315;
Mca-PLGL-Dpa-AR-NH2 is a synthetic fluorogenic peptide substrate widely recognized for its utility in protease activity assays, particularly those involving matrix metalloproteinases (MMPs) and related enzymes. Featuring a unique sequence with a 7-methoxycoumarin-4-acetyl (Mca) fluorophore and a 3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl (Dpa) quencher, this compound offers sensitive detection through fluorescence resonance energy transfer (FRET). The peptide's design allows for efficient cleavage by specific proteases, resulting in a measurable increase in fluorescence, making it highly valuable for kinetic studies and high-throughput screening. Its stability and specificity also contribute to its popularity in both academic and industrial research settings, where precise enzyme monitoring is critical for biochemical investigations.
Enzyme Kinetics and Mechanistic Studies: Mca-PLGL-Dpa-AR-NH2 serves as an indispensable tool for characterizing the catalytic properties of proteases, especially MMPs. By incorporating both a fluorophore and a quencher within its structure, the substrate undergoes a significant fluorescence shift upon enzymatic cleavage, enabling real-time monitoring of proteolytic activity. Researchers utilize this property to determine kinetic parameters such as Km and Vmax, investigate substrate specificity, and explore enzyme-inhibitor interactions. The ability to conduct continuous assays with high sensitivity allows for detailed mechanistic studies, shedding light on enzyme function and regulation in complex biological systems.
High-Throughput Inhibitor Screening: In the context of drug discovery and biochemical screening, this FRET-based peptide substrate is instrumental in identifying and characterizing protease inhibitors. Its robust fluorescence response upon cleavage enables rapid and reliable quantification of enzyme activity in microplate formats, making it suitable for high-throughput screening campaigns. Scientists can efficiently evaluate large libraries of small molecules or biologics for their inhibitory effects on target proteases, accelerating the identification of lead compounds and facilitating structure-activity relationship studies. The substrate's compatibility with automated platforms further streamlines the screening process, supporting the development of novel therapeutic agents targeting proteolytic enzymes.
Protease Profiling in Biological Samples: The substrate is frequently employed to assess protease activity in complex biological matrices, such as cell lysates, tissue extracts, or conditioned media. Its sensitivity and specificity allow researchers to detect and quantify active proteases under various physiological or pathological conditions. This application is particularly valuable in studies investigating the role of proteases in tissue remodeling, inflammation, or cancer progression, where changes in enzyme activity can provide insights into underlying biological processes. By enabling the profiling of proteolytic activity in situ, the substrate contributes to a deeper understanding of enzyme function in health and disease.
Biochemical Pathway Elucidation: Mca-PLGL-Dpa-AR-NH2 facilitates the dissection of protease-mediated signaling pathways by providing a direct readout of enzyme activity in response to experimental manipulations. Researchers can monitor how genetic modifications, pharmacological treatments, or environmental stimuli affect protease function, thereby elucidating the regulatory networks that govern cellular behavior. The substrate's rapid and quantitative response supports time-course experiments and dose-response analyses, making it a versatile reagent for mapping biochemical pathways and identifying key regulatory nodes.
Enzyme Engineering and Mutagenesis Studies: The peptide substrate is also valuable in the field of protein engineering, where it is used to evaluate the functional consequences of site-directed mutagenesis or enzyme redesign. By measuring changes in substrate cleavage efficiency, scientists can assess the impact of specific amino acid substitutions on protease activity and substrate recognition. This approach enables the rational design of enzymes with altered specificity or enhanced catalytic properties, advancing applications in biotechnology and synthetic biology. The substrate's well-defined cleavage site and fluorescence-based detection make it an ideal choice for iterative cycles of mutagenesis and screening, supporting the development of tailored proteolytic tools for diverse research needs.
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