Set2 Activators
Set2 activators, as a chemical class, predominantly operate by influencing the delicate balance of histone modifications, specifically methylation. By targeting various enzymes responsible for these modifications, these activators can indirectly enhance or emphasize the activity of Set2, a histone methyltransferase responsible for the methylation of histone H3 at lysine 36 (H3K36me). For instance, histone acetyltransferase like C646 and HDAC such as MS-275 and Mocetinostat modulate the acetylation landscape of histones. This interplay between acetylation and methylation sets the stage for Set2's activity, as changes in histone acetylation can indirectly influence its ability to methylate H3K36.
Similarly, targeting other histone methyltransferases, such as EPZ004777 and BIX-01294 (targeting G9a and associated enzymes), or those like DZNep, GSK126, and EPZ-6438 (focusing on EZH2 and H3K27 methylation), play a pivotal role. By modifying the histone methylation landscape-specifically at residues like H3K9 or H3K27-these activators create an environment where Set2's methylation activity can be indirectly accentuated. In essence, Set2 activators work not by directly enhancing the enzyme's function but by subtly altering the chromatin context, thereby spotlighting Set2's crucial role in transcriptional elongation and the broader genomic orchestration.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
MS-275 | 209783-80-2 | sc-279455 sc-279455A sc-279455B | 1 mg 5 mg 25 mg | $24.00 $90.00 $212.00 | 24 | |
HDAC inhibitor that affects histone acetylation. By modulating the histone acetylation landscape, it can indirectly influence Set2's ability to methylate its specific histone target, possibly elevating H3K36 methylation. | ||||||
Epz004777 | 1338466-77-5 | sc-507560 | 100 mg | $575.00 | ||
DOT1L inhibitor. With DOT1L inhibited, there's a potential shift in the histone methylation landscape. Set2's activity on H3K36 can be indirectly enhanced, ensuring transcriptional regulation. | ||||||
BIX01294 hydrochloride | 1392399-03-9 | sc-293525 sc-293525A sc-293525B | 1 mg 5 mg 25 mg | $37.00 $112.00 $408.00 | ||
Inhibitor of G9a methyltransferase. By decreasing H3K9 methylation, the relative levels of H3K36 methylation by Set2 can be indirectly influenced, ensuring the balance of transcriptional repression and elongation. | ||||||
Mocetinostat | 726169-73-9 | sc-364539 sc-364539B sc-364539A | 5 mg 10 mg 50 mg | $214.00 $247.00 $1463.00 | 2 | |
HDAC inhibitor that alters the acetylation landscape of histones. Through this modulation, Set2's methylation activity can be indirectly enhanced due to the dynamic interplay between methylation and acetylation on histones. | ||||||
Parthenolide | 20554-84-1 | sc-3523 sc-3523A | 50 mg 250 mg | $81.00 $306.00 | 32 | |
Inhibits NF-κB and can influence chromatin remodeling. By altering chromatin dynamics, it might indirectly facilitate Set2's access to its substrate, enhancing H3K36 methylation. | ||||||
3-Deazaneplanocin, HCl salt | 120964-45-6 | sc-351856 sc-351856A sc-351856B | 1 mg 5 mg 10 mg | $256.00 $612.00 $936.00 | 2 | |
Inhibitor of EZH2, targeting H3K27 methylation. Modulating the levels of H3K27me can indirectly shift the methylation balance, allowing Set2 to play a more dominant role in H3K36 methylation. | ||||||
EX 527 | 49843-98-3 | sc-203044 | 5 mg | $87.00 | 32 | |
Inhibits SIRT1 deacetylase. With altered histone acetylation, Set2's activity can be indirectly influenced due to the complex relationship between acetylation and methylation. | ||||||
EPZ6438 | 1403254-99-8 | sc-507456 | 1 mg | $66.00 | ||
Another EZH2 inhibitor. Altering the H3K27 methylation can result in an indirect compensation by Set2, emphasizing its role in H3K36 methylation. | ||||||