The ASXL2 Activators are a group of chemical compounds specifically selected for their potential to enhance the functional activity of ASXL2, which is intricately involved in chromatin remodeling and the regulation of gene expression. DNA methyltransferase inhibitors like 5-Aza-2'-deoxycytidine and RG108 are pivotal as they may amplify ASXL2's influence on epigenetic mechanisms governing gene expression. Similarly, histone deacetylase inhibitors such as Trichostatin A, Vorinostat, MS-275, and Panobinostat are crucial for potentially augmenting ASXL2's role in histone modification and chromatin restructuring, thereby influencing transcriptional regulation.
Compounds targeting specific histone methyltransferases like GSK126 (EZH2 inhibitor), BIX-01294, and UNC1999, provide a strategic approach to modulate interactions between ASXL2 and components of the polycomb repressive complex 2, crucial in histone methylation and gene silencing. The inclusion of JQ1, a BET bromodomain inhibitor, along with the Menin-MLL inhibitor, underlines the importance of ASXL2 in broader chromatin organization and gene expression processes. EPZ-6438, a selective EZH2 inhibitor, further emphasizes the role of ASXL2 in the context of chromatin dynamics and epigenetic regulation.
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