MC(C5)-Val-Cit integrates a cleavable linker with hydrophobic and polar domains that inform enzymatic recognition studies. The Val-Cit motif enables selective cleavage analysis in controlled environments. Researchers evaluate its stability and solubility across conditions. Applications include prodrug-linker modeling, kinetic research, and peptide conjugation strategies.
CAT No: R2652
CAS No:2504147-59-3
Synonyms/Alias:MC(C5)-Val-Cit;2504147-59-3;(5-(2,5-DIOXO-2,5-DIHYDRO-1H-PYRROL-1-YL)PENTANOYL)-L-VALYL-L-ARGININE;(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[5-(2,5-dioxopyrrol-1-yl)pentanoylamino]-3-methylbutanoyl]amino]pentanoic acid;MC (C5)-Val-Cit-OH;AKOS040743567;AT10815;HY-141143;CS-0115749;
MC(C5)-Val-Cit is a synthetic peptide linker frequently utilized in the development of antibody-drug conjugates (ADCs) and targeted delivery systems. Structurally, it features a maleimidocaproyl (MC) group connected via a pentyl spacer (C5) to a dipeptide sequence of valine and citrulline (Val-Cit), forming a cleavable linker with precise enzymatic sensitivity. Its core significance lies in its capacity to facilitate the controlled release of payloads within specific biological environments, particularly those where cathepsin B or related proteases are active. This biochemical property makes it a valuable tool in the advancement of selective drug delivery strategies, conjugation chemistry, and mechanistic studies of linker stability and cleavage.
Antibody-Drug Conjugate Research: The Val-Cit dipeptide motif within this linker is recognized for its selective cleavage by lysosomal proteases, notably cathepsin B, which are often upregulated in certain pathological tissues. This property is harnessed in ADC research to enable site-specific release of cytotoxic agents upon internalization by target cells. Researchers employ the MC(C5)-Val-Cit linker to conjugate small molecule drugs to antibodies, optimizing the balance between systemic stability and intracellular payload release, a critical factor in ADC efficacy and safety profiling.
Bioconjugation and Payload Attachment: The maleimidocaproyl group at one end of the linker provides a thiol-reactive site, facilitating stable covalent attachment to cysteine residues on proteins, peptides, or other biomolecules. This functional group allows for efficient and selective conjugation under mild conditions, supporting the generation of homogeneous bioconjugates. In technical workflows, the use of this linker streamlines the assembly of complex molecular constructs with well-defined stoichiometry and predictable in vivo behavior.
Enzyme-Sensitive Linker Mechanism Studies: The MC(C5)-Val-Cit linker serves as a model system for investigating enzyme-mediated cleavage mechanisms in vitro and in cell-based assays. Its well-characterized substrate specificity enables detailed analysis of protease activity, substrate recognition, and cleavage kinetics. Such studies are instrumental in designing next-generation linkers with tailored stability profiles and improved selectivity for targeted drug delivery platforms.
Targeted Delivery System Development: Beyond ADCs, this linker is employed in the broader context of targeted delivery systems, including polymer-drug conjugates and nanoparticle formulations. Its enzymatically cleavable nature allows researchers to engineer delivery vehicles that respond to specific intracellular or extracellular cues, enhancing payload release profiles and minimizing off-target effects. The pentyl spacer in the linker design further contributes to optimizing spatial orientation and accessibility of the cleavage site within macromolecular assemblies.
Analytical and Quality Control Applications: The defined structure and cleavage characteristics of the MC(C5)-Val-Cit linker make it a useful standard in analytical method development for conjugate characterization. It is utilized in mass spectrometry, HPLC, and other analytical platforms to assess conjugation efficiency, linker stability, and payload release kinetics. These analytical applications are essential for process optimization, quality control, and regulatory documentation in the development of bioconjugate-based research tools and investigational products.
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