L3MBTL3 Inhibitors
Chemical inhibitors of L3MBTL3 utilize various mechanisms to impede the protein's ability to modulate chromatin structure and function. UNC1215, for instance, competes with natural ligands for binding to the MBT domain of L3MBTL3, effectively blocking the protein's interaction with methylated lysine residues on histones. This interruption of binding prevents L3MBTL3 from exerting its role in chromatin compaction and gene expression regulation. Similarly, UNC1679 operates by engaging the MBT domain of L3MBTL3 with greater potency and selectivity than UNC1215, providing a more pronounced inhibition of the protein's chromatin-modifying activities. These molecules directly target the functional domain of L3MBTL3, rendering it incapable of recognizing and binding to its specific histone marks.
Additionally, several other inhibitors indirectly influence L3MBTL3 function by modifying the histone landscape. For instance, MS023 inhibits type I protein arginine methyltransferases (PRMTs), which are involved in the methylation of arginine residues on histones. This reduction in methylated arginine residues consequently diminishes the substrates available for L3MBTL3 to bind. GSK343, on the other hand, specifically inhibits EZH2 methyltransferase, thereby reducing the trimethylation of histone H3 lysine 27 (H3K27me3) and potentially decreasing the affinity of L3MBTL3 for these marks. IOX1 targets a broader range of 2-oxoglutarate (2OG) dependent dioxygenases, enzymes that modify various histone and non-histone proteins, potentially leading to a decrease in L3MBTL3's chromatin-reading ability. Similarly, SGC707 and LLY-507 inhibit PRMT5 and SMYD2, respectively, which are enzymes that methylate arginine and lysine residues recognized by L3MBTL3, thereby indirectly impeding the protein's interaction with methylated chromatin. Lastly, PFI-2 specifically inhibits SETD7, leading to a decrease in monomethylated lysine 4 on histone H3, a known binding site for L3MBTL3, further inhibiting the protein's ability to interact with chromatin. These chemical inhibitors collectively disrupt the chromatin-modifying functions of L3MBTL3 by altering the availability or recognition of its methylated histone substrates.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
UNC 1215 | 1415800-43-9 | sc-475020 | 10 mg | $380.00 | ||
UNC1215 is a chemical inhibitor that binds competitively to the MBT domain of L3MBTL3, which is responsible for recognizing and interacting with mono- and dimethylated lysines. By binding to this domain, UNC1215 inhibits the protein's ability to bind to its methyl-lysine histone marks, thereby inhibiting L3MBTL3's chromatin-modifying functions. | ||||||
MS023 | 1831110-54-3 | sc-507463 | 5 mg | $165.00 | ||
MS023 is a type I protein arginine methyltransferase (PRMT) inhibitor that would inhibit PRMTs involved in methylating histone or non-histone proteins. Since L3MBTL3 recognizes methylated lysine residues, the inhibition of PRMTs by MS023 would result in a decrease in substrates available for L3MBTL3 to bind, thereby functionally inhibiting its chromatin-modifying activity. | ||||||
GSK343 | 1346704-33-3 | sc-397025 sc-397025A | 5 mg 25 mg | $148.00 $452.00 | 1 | |
GSK343 is an EZH2 methyltransferase inhibitor which reduces the trimethylation of histone H3 at lysine 27 (H3K27me3). As L3MBTL3 can bind methylated lysines, altering the methylation status of histones with GSK343 could reduce the binding opportunities for L3MBTL3, thereby inhibiting its ability to contribute to chromatin compaction and gene regulation. | ||||||
SGC707 | 1687736-54-4 | sc-507461 | 1 mg | $48.00 | ||
SGC707 is an inhibitor of protein arginine methyltransferase 5 (PRMT5). PRMT5 is responsible for symmetric dimethylation of arginine residues on histones. By inhibiting PRMT5, SGC707 reduces the methylated arginine marks recognized by L3MBTL3, which in turn inhibits the protein's ability to modify chromatin structure and regulate gene expression. | ||||||
Epz004777 | 1338466-77-5 | sc-507560 | 100 mg | $575.00 | ||
EPZ004777 is a selective inhibitor of the histone methyltransferase DOT1L. Although L3MBTL3 does not directly interact with the methylation marks introduced by DOT1L, the widespread changes in the chromatin landscape caused by DOT1L inhibition could indirectly affect the binding and function of L3MBTL3, inhibiting its role in chromatin compaction and gene expression. | ||||||