Unc3866 is a designed peptidomimetic containing aromatic, aliphatic, and basic residues that contribute to strong secondary-structure preferences. Researchers use it to examine protein-peptide interfaces, helix alignment, and hydrophobic packing. The molecule's modular design supports structure-activity exploration. Its stability aids high-resolution biochemical assays.
CAT No: R2309
CAS No:1872382-47-2
Synonyms/Alias:UNC3866;1872382-47-2;(3S,6S,9S,12S,15S)-Methyl 3-benzyl-1-(4-(tert-butyl)phenyl)-12-(4-(diethylamino)butyl)-15-(hydroxymethyl)-9-isobutyl-6-methyl-1,4,7,10,13-pentaoxo-2,5,8,11,14-pentaazahexadecan-16-oate;CHEMBL3939958;methyl N2-(4-(tert-butyl)benzoyl)-L-phenylalanyl-L-alanyl-L-leucyl-N6,N6-diethyl-L-lysyl-L-serinate;UNC-3866;methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-tert-butylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-(diethylamino)hexanoyl]amino]-3-hydroxypropanoate;UNC 3866;SCHEMBL23682865;EX-A1501;XZC38247;BDBM50194259;s8359;AKOS030632022;CCG-270488;CS-6101;AC-36145;BS-16367;DA-68478;N-[4-(1,1-Dimethylethyl)benzoyl]-L-phenylalanyl-L-alanyl-L-leucyl-N6,N6-diethyl-L-lysyl-L-serine methyl ester;HY-100832;D84021;methyl (2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(4-tert-butylphenyl)formamido]-3-phenylpropanamido]propanamido]-4-methylpentanamido]-6-(diethylamino)hexanamido]-3-hydroxypropanoate;
Unc3866 is a synthetic peptide-based ligand that functions as a potent and selective inhibitor of methyl-lysine reader proteins, particularly those belonging to the chromodomain family such as CBX7 and CBX4. As a rationally designed chemical probe, it has become an important tool in epigenetics research, enabling the interrogation of protein-protein interactions involved in chromatin remodeling and gene regulation. Its unique structure mimics methylated lysine residues, allowing specific binding to chromodomain-containing proteins and facilitating the study of their biological roles. Unc3866's high selectivity and cell-permeable characteristics make it especially valuable for dissecting the functions of Polycomb group proteins and their contributions to transcriptional repression and cellular identity.
Epigenetic Mechanism Elucidation: Unc3866 is widely utilized in studies aiming to unravel the molecular mechanisms governing chromatin dynamics and epigenetic regulation. By selectively inhibiting CBX chromodomains, researchers can dissect how methyl-lysine reader proteins recognize post-translational histone modifications and mediate transcriptional silencing. This approach enables precise mapping of protein-DNA and protein-protein interactions within Polycomb repressive complexes, offering new insights into the orchestration of gene expression patterns during development and differentiation.
Chemical Probe Validation: As a benchmark chemical probe, Unc3866 is instrumental in validating the functional importance of chromodomain interactions in various biological systems. Its use in competitive binding assays, pull-down experiments, and co-immunoprecipitation studies allows for the selective disruption of chromodomain-histone interactions, helping to define the specificity and biological consequences of these epigenetic readers. Such validation is critical for distinguishing direct targets from off-target effects in complex cellular environments.
Chromatin Immunoprecipitation (ChIP) Studies: The compound's ability to disrupt chromodomain binding to methylated histones makes it a valuable tool in chromatin immunoprecipitation protocols. By pre-treating cells or chromatin extracts with Unc3866, researchers can assess the dependency of protein localization at specific genomic loci on chromodomain-mediated recognition. This strategy enables functional dissection of Polycomb complex recruitment and helps clarify the relationship between histone modifications and gene repression at the chromatin level.
Cellular Pathway Analysis: Unc3866 is frequently employed to probe the downstream effects of chromodomain inhibition on cellular signaling pathways and transcriptional networks. Through transcriptomic profiling and phenotypic assays following treatment, scientists can characterize the broader regulatory roles of Polycomb group proteins in maintaining cell fate, lineage specification, and response to environmental cues. These studies contribute to a deeper understanding of how epigenetic modifications integrate with cellular signaling to control gene expression programs.
Small Molecule Screening and Drug Discovery: The well-characterized binding properties and selectivity profile of Unc3866 make it an ideal reference compound in high-throughput screening campaigns aimed at discovering novel modulators of methyl-lysine reader proteins. Its use in structure-activity relationship (SAR) studies facilitates the identification and optimization of new chemical entities targeting chromodomains, thereby advancing early-stage drug discovery efforts focused on epigenetic regulators. This application underscores the compound's value not only as a research tool but also as a standard for benchmarking new inhibitors in the field of chemical biology.
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