BAZ2B Activators
BAZ2B Activators are chemical compounds that, indirectly, can enhance the functional activity of BAZ2B, a protein involved in reading epigenetic marks and influencing chromatin structure and gene expression. Since there are no known direct activators of BAZ2B, the focus is on compounds that modify the epigenetic landscape to which BAZ2B responds. Compounds such as EZH2 inhibitors (EPZ-6438, GSK126, CPI-169) reduce the methylation of H3K27, a repressive mark that BAZ2B can bind to. With fewer sites bearing this mark, BAZ2B's recruitment to these repressive regions may be decreased, which could result in increased activity in transcriptionally active parts of the chromatin.
The other class of compounds listed,including BET bromodomain inhibitors (PFI-1, RVX-208, I-BET151), Jumonji demethylase inhibitors (JIB-04), methyllysine reader antagonists (UNC1215), and methyltransferase inhibitors (LLY-507, A-366), all work by altering the chromatin landscape. For instance, BET inhibitors displace BET proteins from acetylated lysines, potentially increasing the availability of these sites for BAZ2B to bind and activate transcription. HDAC inhibitors prevent the deacetylation of histones, fostering an open chromatin state that could enhance BAZ2B's chromatin engagement. Similarly, inhibitors of methyltransferases like SMYD2 and G9a/GLP reduce specific methylation marks, potentially allowing BAZ2B to access and influence these regions more effectively.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
EPZ6438 | 1403254-99-8 | sc-507456 | 1 mg | $66.00 | ||
EPZ-6438 is an inhibitor of the enhancer of zeste homolog 2 (EZH2) methyltransferase, which results in decreased methylation of histone H3 at lysine 27 (H3K27me3). By reducing this repressive mark, BAZ2B, which reads methyl marks, may be recruited less to chromatin, thus enhancing its availability for transcriptional activation elsewhere. | ||||||
GSK126 | 1346574-57-9 | sc-490133 sc-490133A sc-490133B | 1 mg 5 mg 10 mg | $92.00 $243.00 $306.00 | ||
GSK126 is another EZH2 methyltransferase inhibitor, leading to a reduction in H3K27me3 levels. This alters chromatin states, potentially enhancing BAZ2B's ability to bind to less densely packed chromatin regions, promoting transcriptional activation. | ||||||
JIB 04 | 199596-05-9 | sc-397040 | 20 mg | $177.00 | ||
JIB-04 is a pan-inhibitor of Jumonji demethylases, which are responsible for removing methyl groups from histones. Inhibition of these enzymes can lead to an indirect enrichment of histone methylation marks that BAZ2B could interpret as signals for transcriptional activation. | ||||||
UNC 1215 | 1415800-43-9 | sc-475020 | 10 mg | $380.00 | ||
UNC1215 is a selective antagonist of the methyllysine reader protein L3MBTL3. By blocking L3MBTL3, it may cause a compensatory increase in the activity of other methyllysine readers such as BAZ2B, thus enhancing its functional engagement with chromatin. | ||||||
PFI-1 | 1403764-72-6 | sc-478504 | 5 mg | $98.00 | ||
PFI-1 is a BET bromodomain inhibitor that prevents the binding of BET proteins to acetylated lysines on histones. This could result in increased availability of these sites for BAZ2B, promoting its role in chromatin remodeling and transcriptional activation. | ||||||
RVX 208 | 1044870-39-4 | sc-472700 | 10 mg | $340.00 | ||
RVX-208 is a BET bromodomain inhibitor. By inhibiting the binding of BET proteins, more chromatin sites may become available for BAZ2B, possibly enhancing its transcriptional activation capacity. | ||||||
I-BET 151 Hydrochloride | 1300031-49-5 (non HCl Salt) | sc-391115 | 10 mg | $450.00 | 2 | |
I-BET151 is a selective inhibitor for BET bromodomains, displacing BET proteins from chromatin. This displacement may enhance the chromatin binding and functional activity of BAZ2B. | ||||||
A-366 | 1527503-11-2 | sc-507495 | 10 mg | $195.00 | ||
A-366 is a selective G9a/GLP histone methyltransferase inhibitor. The reduction in H3K9 methylation could lead to chromatin decondensation, potentially enhancing the transcriptional regulation capabilities of BAZ2B. | ||||||