MM-401 TFA is a peptide-derived inhibitor scaffold widely used to probe histone methyltransferase recognition and chromatin-associated interactions. Its sequence mimics key lysine-containing motifs within histone tails. Researchers investigate binding thermodynamics, structural rearrangements, and epigenetic complex formation. Applications span chromatin biochemistry, probe development, and structure-activity relationship analysis.
CAT No: R2692
CAS No:1442106-11-7
Synonyms/Alias:MM-401 TFA;1442106-11-7;MM-401 (TFA);CHEMBL4099772;HY-19554A;DA-65550;CS-0104334;F82461;N-[(3R,6S,9S,12R)-9-[3-(diaminomethylideneamino)propyl]-6-ethyl-12-methyl-2,5,8,11-tetraoxo-3-phenyl-1,4,7,10-tetrazacyclohexadec-12-yl]-2-methylpropanamide;2,2,2-trifluoroacetic acid;
MM-401 Tfa is a synthetic carbohydrate compound that has garnered significant attention in the field of chemical biology and epigenetic research. Characterized by its unique structural properties, MM-401 Tfa is primarily utilized as a potent and selective inhibitor targeting the mixed-lineage leukemia (MLL1) protein complex. Its molecular design enables researchers to probe the regulatory mechanisms of histone methylation with high specificity, making it a valuable tool for dissecting the intricate networks of gene expression modulation. The compound's compatibility with a wide range of experimental platforms, including in vitro enzymatic assays and cell-based studies, further underscores its versatility for scientific exploration.
Epigenetic Mechanism Studies: MM-401 Tfa plays a pivotal role in advancing the understanding of histone modification processes, particularly those involving the methylation of histone H3 lysine 4 (H3K4). By selectively inhibiting the MLL1-WDR5 interaction, it allows scientists to delineate the downstream effects of disrupted methyltransferase activity on chromatin structure and gene transcription. This targeted approach provides a robust foundation for unraveling the complexities of epigenetic regulation and its impact on cellular identity and function. Researchers can utilize this compound to investigate the dynamic interplay between chromatin modifiers and transcription factors, thereby elucidating the fundamental principles of gene regulation at the molecular level.
Drug Discovery and Target Validation: In the realm of pharmaceutical research, MM-401 Tfa serves as an essential chemical probe for validating MLL1 as a potential therapeutic target. By modulating the activity of this key epigenetic regulator, it enables high-throughput screening platforms to assess the efficacy of novel small molecules in preclinical models. Its application facilitates the identification of lead compounds with desirable pharmacological profiles, accelerating the drug discovery pipeline. Furthermore, it aids in the characterization of off-target effects and the optimization of candidate molecules, thereby streamlining the development of targeted therapies for various pathological conditions associated with aberrant epigenetic signaling.
Cancer Biology Research: The study of malignant transformation and tumor progression often necessitates precise tools to manipulate gene expression pathways. MM-401 Tfa, through its inhibitory action on the MLL1 complex, empowers researchers to explore the contribution of epigenetic dysregulation to oncogenic processes. By disrupting the maintenance of active chromatin states at critical gene loci, the compound provides insights into the molecular drivers of uncontrolled cell proliferation and survival. Its use in cancer biology extends to the investigation of resistance mechanisms, enabling the development of innovative strategies to overcome therapeutic challenges in oncology research.
Stem Cell Differentiation: In developmental biology and regenerative medicine, MM-401 Tfa is employed to investigate the role of histone methylation in stem cell fate determination. By perturbing the enzymatic function of MLL1, it allows for the controlled modulation of gene expression programs that govern lineage commitment and cellular plasticity. This application is particularly valuable for elucidating the epigenetic cues that orchestrate differentiation processes, thereby informing strategies for the directed differentiation of pluripotent stem cells and the generation of specialized cell types for research and therapeutic purposes.
Transcriptional Regulation Analysis: The ability to selectively inhibit the MLL1 complex with MM-401 Tfa provides a powerful means to study the transcriptional networks underlying cellular responses to environmental cues. Researchers can employ this compound to dissect the contribution of H3K4 methylation to the activation or repression of target genes in various biological contexts. By integrating transcriptomic and epigenomic profiling techniques, it is possible to map the global changes in gene expression landscapes induced by the inhibition of MLL1 activity. This comprehensive approach enhances the understanding of how chromatin modifications integrate with signaling pathways to orchestrate complex cellular behaviors, ultimately advancing the broader field of gene regulation research.
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