EZHIP Inhibitors
EZHIP inhibitors are a class of chemical compounds that specifically target the EZHIP (EZH Inhibitory Protein) protein, which is known to play a regulatory role in chromatin structure and gene expression. EZHIP is particularly involved in the inhibition of the polycomb repressive complex 2 (PRC2), a critical protein complex responsible for catalyzing the trimethylation of lysine 27 on histone H3 (H3K27me3). This modification is a key epigenetic mark that contributes to the repression of gene expression. By inhibiting EZHIP, these compounds disrupt its interaction with PRC2, which may lead to changes in histone methylation patterns and alterations in chromatin states. This makes EZHIP inhibitors important tools for studying the regulation of chromatin dynamics and the role of histone modifications in gene expression.
The chemical structure of EZHIP inhibitors is designed to target specific domains of the EZHIP protein, often aiming to block its ability to interact with PRC2 or disrupt its inhibitory function. These inhibitors can bind to EZHIP's functional motifs, preventing its association with histone-modifying enzymes and thereby altering the downstream effects on chromatin compaction and accessibility. Researchers use EZHIP inhibitors to explore the biological functions of EZHIP in maintaining chromatin organization and regulating gene silencing across different cell types. The inhibition of EZHIP provides insights into how chromatin remodeling affects processes such as differentiation, development, and gene silencing mechanisms. Overall, these inhibitors serve as valuable chemical tools for understanding the complexities of epigenetic regulation and chromatin-based gene control.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
GSK126 | 1346574-57-9 | sc-490133 sc-490133A sc-490133B | 1 mg 5 mg 10 mg | $90.00 $238.00 $300.00 | ||
GSK126 is a potent and highly selective inhibitor of EZH2 methyltransferase activity, a core component of PRC2, which results in a decrease in H3K27me3 levels. Since EZHIP functions by inhibiting the methyltransferase activity of PRC2, GSK126’s suppression of PRC2 enzymatic activity would obviate the need for EZHIP's inhibitory function, effectively diminishing EZHIP's role. | ||||||
UNC1999 | 1431612-23-5 | sc-475314 | 5 mg | $142.00 | 1 | |
UNC1999 is a selective inhibitor of EZH2 and EZH1, which are methyltransferases in the PRC2 complex. By inhibiting these enzymes, UNC1999 directly reduces the methylation of histone H3 at Lys27. As EZHIP works to block this same methylation process, the presence of UNC1999 would render the inhibitory effects of EZHIP on PRC2 redundant, hence indirectly diminishing its functional significance. | ||||||
EPZ6438 | 1403254-99-8 | sc-507456 | 1 mg | $66.00 | ||
EPZ-6438, also known as Tazemetostat, inhibits EZH2, a histone-lysine N-methyltransferase enzyme, which leads to a decrease in histone H3K27 methylation. With the inhibition of EZH2, the methylation that EZHIP seeks to inhibit is already reduced, thereby indirectly inhibiting the functional necessity of EZHIP. | ||||||
GSK343 | 1346704-33-3 | sc-397025 sc-397025A | 5 mg 25 mg | $148.00 $452.00 | 1 | |
GSK343 is a selective and potent inhibitor of EZH2, leading to a reduction in H3K27 methylation. This compound, by inhibiting EZH2, diminishes the role of EZHIP in acting as an inhibitor of the PRC2 complex, thus indirectly inhibiting the functional significance of EZHIP in the cell. | ||||||
UNC0638 | 1255580-76-7 | sc-397012 | 10 mg | $315.00 | ||
UNC0638 is an inhibitor of G9a and GLP, which are histone lysine methyltransferases responsible for the methylation of H3K9. Although EZHIP is specifically an inhibitor of PRC2, changes in the methylation status of other histone residues, such as H3K9, could affect chromatin structure and indirectly influence the functional context in which EZHIP operates, leading to an indirect inhibition of its activity. | ||||||
MS-275 | 209783-80-2 | sc-279455 sc-279455A sc-279455B | 1 mg 5 mg 25 mg | $24.00 $88.00 $208.00 | 24 | |
MS-275, also known as Entinostat, is a class I histone deacetylase inhibitor. By altering the acetylation status of histones, MS-275 can affect chromatin structure and thus indirectly impact the function of chromatin-associated proteins, including EZHIP. Since EZHIP's role is related to the modification status of histones, changes in acetylation levels could alter the effectiveness of EZHIP's inhibitory action on PRC2. | ||||||