Menin Inhibitors
Menin inhibitors encompass a range of compounds that indirectly modulate the biological function of Menin through alteration of its interaction networks and the chromatin landscape. Since Menin is an essential component of the histone methyltransferase complex associated with PRC2, compounds like BRD4770, 3-Deazaneplanocin A, DZNep, GSK343, EPZ-6438, UNC1999, CPI-1205, GSK126, and LLY-507, which target the methylation processes, may influence the transcriptional regulation activities of Menin. Menin's role is not solely limited to transcriptional regulation; it is also crucial for maintaining genome stability, therefore, changes in histone modification patterns brought about by these compounds can indirectly affect Menin's functions.
The histone methyltransferases, such as SMYD2, G9a, GLP, and SUV39H1, are significant for the regulation of gene expression through epigenetic modifications. Menin is known to associate with transcriptional regulators, and its ability to regulate gene expression can be indirectly influenced by inhibitors like LLY-507, BIX-01294, Chaetocin, and A-366 that target these methyltransferases. By modulating the activity of these enzymes, the associated inhibitors can affect the epigenetic marks that Menin may utilize to exert its functions in chromatin remodeling and gene expression. These indirect mechanisms of Menin inhibition emphasize the intricate interplay between chromatin state and transcriptional control, where Menin operates at the confluence of these fundamental cellular processes.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
GSK343 | 1346704-33-3 | sc-397025 sc-397025A | 5 mg 25 mg | $151.00 $461.00 | 1 | |
GSK343 is an EZH2 selective inhibitor that suppresses the histone methyltransferase activity of PRC2, a complex that Menin associates with, altering transcriptional outcomes. | ||||||
EPZ6438 | 1403254-99-8 | sc-507456 | 1 mg | $66.00 | ||
EPZ-6438 (Tazemetostat) inhibits EZH2, and by extension, could disrupt Menin's role in the PRC2 complex, affecting its function in gene expression regulation. | ||||||
UNC1999 | 1431612-23-5 | sc-475314 | 5 mg | $142.00 | 1 | |
UNC1999 is a selective inhibitor of EZH1/2, which are part of the PRC2 complex, potentially interfering with Menin's regulatory roles in chromatin modification. | ||||||
GSK126 | 1346574-57-9 | sc-490133 sc-490133A sc-490133B | 1 mg 5 mg 10 mg | $92.00 $243.00 $306.00 | ||
As an inhibitor of EZH2, GSK126 can impact the histone methyltransferase activity of the PRC2 complex and consequently affect Menin's co-regulatory functions. | ||||||
Histone Lysine Methyltransferase Inhibitor Inhibitor | 935693-62-2 (free base) | sc-202651 | 5 mg | $151.00 | 4 | |
BIX-01294 inhibits G9a and GLP histone lysine methyltransferases, potentially disrupting interactions with Menin that facilitate transcriptional repression. | ||||||
Chaetocin | 28097-03-2 | sc-200893 | 200 µg | $126.00 | 5 | |
By inhibiting the histone methyltransferase SUV39H1, chaetocin could impact chromatin structures where Menin functions in genome stability. | ||||||
A-366 | 1527503-11-2 | sc-507495 | 10 mg | $195.00 | ||
A selective G9a/GLP inhibitor that may affect Menin's role in chromatin remodeling and transcriptional regulation by altering histone methylation. | ||||||