ASH2L Activators
ASH2L activators are a class of chemical compounds that enhance the functional activity of ASH2L through their roles in influencing the methylation landscape of histones.ASH2L is a part of the mixed lineage leukemia (MLL) complex, which is responsible for the methylation of histone H3 at lysine 4 (H3K4), an active chromatin mark. Some compounds function as inhibitors of enzymes that add repressive marks to histones or DNA, such as G9a or DNA methyltransferases. For instance, Bix-01294 inhibits G9a histone methyltransferase, facilitating H3K4 methylation by the MLL complex, while RG108 prevents DNA methylation, indirectly enhancing ASH2L's activity. Other compounds specifically target the competition for H3K4 methylation sites. EPZ004777 and EPZ-5676, which inhibit DOT1L, favor H3K4 methylation by reducing H3K79 methylation, a competing process.
Compounds like PFI-2 and GSK126 inhibit other histone methyltransferases like SETD7 and EZH2, respectively, reducing the competition for H3K4 methylation sites and enhancing ASH2L's functional activity. Anacardic Acid and Chaetocin, on the other hand, are non-specific inhibitors of histone methyltransferases but can still enhance the activity of ASH2L by reducing competition for H3K4 methylation sites. Some activators, such as Mocetinostat and Parthenolide, operate by inhibiting processes that generally favor gene repression, like histone deacetylation or NF-κB activation. This favors the methylation of H3K4 over repressive gene regulatory mechanisms, indirectly enhancing ASH2L's activity. The common thread among all these compounds is their ability to alter the chromatin landscape in a way that favors the functional activity of ASH2L, underlining their potential as ASH2L activators.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
BIX01294 hydrochloride | 1392399-03-9 | sc-293525 sc-293525A sc-293525B | 1 mg 5 mg 25 mg | $36.00 $110.00 $400.00 | ||
Bix-01294 is a G9a histone methyltransferase (HMTase) inhibitor. ASH2L is part of the mixed lineage leukemia (MLL) complex, which is responsible for the methylation of histone H3 at lysine 4 (H3K4). By inhibiting G9a HMTase, Bix-01294 can counteract the methylation of H3K9, a repressive mark, thereby favoring the H3K4 methylation and enhancing the functional activity of ASH2L. | ||||||
Epz004777 | 1338466-77-5 | sc-507560 | 100 mg | $575.00 | ||
EPZ004777 is a selective inhibitor of the DOT1L methyltransferase. DOT1L is responsible for H3K79 methylation, which can compete with H3K4 methylation. Inhibition of DOT1L by EPZ004777 can therefore enhance the methylation activity of ASH2L on H3K4. | ||||||
RG 108 | 48208-26-0 | sc-204235 sc-204235A | 10 mg 50 mg | $128.00 $505.00 | 2 | |
RG108 is a DNA methyltransferase inhibitor. By inhibiting DNA methylation, RG108 can prevent the silencing of genes. This may indirectly enhance the activity of ASH2L by favoring the methylation of H3K4, an active mark, over DNA methylation, a repressive mark. | ||||||
Chaetocin | 28097-03-2 | sc-200893 | 200 µg | $120.00 | 5 | |
Chaetocin is a non-specific inhibitor of HMTases. Although it inhibits HMTases generally, its use can favor the methylation of H3K4 by ASH2L, as this process is not affected by chaetocin. | ||||||
Sinefungin | 58944-73-3 | sc-203263 sc-203263B sc-203263C sc-203263A | 1 mg 100 mg 1 g 10 mg | $266.00 $5100.00 $39576.00 $690.00 | 4 | |
Sinefungin is a S-adenosylmethionine (SAM) analog and inhibits various methyltransferases. Despite its general inhibitory effect, sinefungin can enhance the functional activity of ASH2L by reducing competition for SAM, the methyl group donor, thus facilitating H3K4 methylation. | ||||||
Parthenolide | 20554-84-1 | sc-3523 sc-3523A | 50 mg 250 mg | $79.00 $300.00 | 32 | |
Parthenolide is a potent inhibitor of NF-κB activation. By inhibiting NF-κB, which can mediate gene repression, parthenolide may indirectly enhance the functional activity of ASH2L by favoring the methylation of H3K4 over repressive gene regulatory mechanisms. | ||||||
Anacardic Acid | 16611-84-0 | sc-202463 sc-202463A | 5 mg 25 mg | $100.00 $200.00 | 13 | |
Anacardic acid inhibits various HMTases. Although it is a general HMTase inhibitor, anacardic acid can favor the activity of ASH2L by reducing competition for H3K4 methylation sites, thereby enhancing ASH2L's functional activity. | ||||||
9-[5-Deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofuranosyl]-9H-purin-6-amine | 1380288-87-8 | sc-500607 | 50 mg | $13500.00 | ||
EPZ-5676 is a selective inhibitor of DOT1L. By inhibiting DOT1L, which methylates H3K79, EPZ-5676 can favor the methylation of H3K4 by ASH2L, enhancing its functional activity. | ||||||
Mocetinostat | 726169-73-9 | sc-364539 sc-364539B sc-364539A | 5 mg 10 mg 50 mg | $210.00 $242.00 $1434.00 | 2 | |
Mocetinostat is an inhibitor of class I and IV histone deacetylases (HDACs). By inhibiting HDACs, mocetinostat can prevent the deacetylation of histones, a process that generally favors gene repression. This can indirectly enhance ASH2L's activity by favoring the methylation of H3K4, an active mark. | ||||||
UNC0638 | 1255580-76-7 | sc-397012 | 10 mg | $315.00 | ||
UNC0638 is a selective inhibitor of G9a and GLP HMTases. By inhibiting these enzymes, which methylate H3K9, UNC0638 can favor the methylation of H3K4 by ASH2L, enhancing its functional activity. | ||||||