BRWD3 Activators
The activation of BRWD3 is understood to be modulated through its interactions with chromatin, which are influenced by the presence of specific epigenetic marks such as acetylation and methylation. For example, HDAC inhibitors like Panobinostat increase the acetylation levels on histones, which can facilitate the binding of BRWD3's bromodomain to these marks, thereby activating its role in chromatin remodeling and transcriptional regulation. Similarly, DNMT inhibitors, such as 5-Aza-2'-deoxycytidine, reduce methylation levels on DNA, potentially augmenting the activity of BRWD3 in gene regulation by allowing it greater access to chromatin regions that are generally repressed when methylated.
Other compounds, such as EZH2 inhibitors (GSK343), indirectly activate BRWD3 by reducing the presence of repressive methyl marks (H3K27me3), which are associated with condensed, inactive chromatin. Their reduction potentially facilitates a chromatin state that BRWD3 can bind to more effectively, thus participating in the transcriptional activation of genes. Additionally, BET bromodomain inhibitors (CPI-0610, PFI-1) function by competitively inhibiting other bromodomain proteins, which can lead to increased availability of acetylated histones for BRWD3, potentially enhancing its activity in the chromatin context.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
5-Aza-2′-Deoxycytidine | 2353-33-5 | sc-202424 sc-202424A sc-202424B | 25 mg 100 mg 250 mg | $214.00 $316.00 $418.00 | 7 | |
This compound inhibits DNA methyltransferases, which leads to hypomethylation of DNA. Hypomethylated DNA is generally associated with active gene expression, potentially augmenting the recruitment and activation of BRWD3 to these regions to modulate gene expression. | ||||||
Trichostatin A | 58880-19-6 | sc-3511 sc-3511A sc-3511B sc-3511C sc-3511D | 1 mg 5 mg 10 mg 25 mg 50 mg | $149.00 $470.00 $620.00 $1199.00 $2090.00 | 33 | |
Similar to SAHA, Trichostatin A causes hyperacetylation of histones, enhancing the chromatin binding and activation of BRWD3, as its bromodomain preferentially interacts with acetylated lysine residues. | ||||||
Methylstat | 1310877-95-2 | sc-507374 | 10 mg | $480.00 | ||
This inhibitor prevents the demethylation of histones, potentially maintaining or increasing methylation marks that BRWD3 recognizes, thereby activating it to engage with such epigenetic marks for gene expression regulation. | ||||||
CPI-0610 | 1380087-89-7 | sc-507490 | 10 mg | $495.00 | ||
CPI-0610's inhibition of BET proteins can lead to alterations in chromatin, indirectly activating BRWD3 by creating more binding opportunities for it to engage in transcriptional regulation. | ||||||
GSK343 | 1346704-33-3 | sc-397025 sc-397025A | 5 mg 25 mg | $148.00 $452.00 | 1 | |
GSK343 selectively inhibits EZH2, decreasing H3K27me3 marks, which can activate BRWD3 by enabling it to interact with chromatin more effectively and participate in the activation of gene expression. | ||||||
PFI-1 | 1403764-72-6 | sc-478504 | 5 mg | $96.00 | ||
PFI-1's inhibition of BET bromodomains can lead to an open chromatin state, activating BRWD3 by enhancing its binding to acetylated histones and promoting gene regulatory functions. | ||||||
Panobinostat | 404950-80-7 | sc-208148 | 10 mg | $196.00 | 9 | |
As a broad-spectrum HDAC inhibitor, Panobinostat increases histone acetylation, which can activate BRWD3 by improving its chromatin engagement and influence on gene expression patterns. | ||||||