HDA4 Inhibitors
Chemical inhibitors of HDA4 target the enzyme's ability to remove acetyl groups from histone proteins, a critical process in the regulation of gene expression. Trichostatin A, Vorinostat, and Panobinostat function by binding to the active site of HDA4, which is necessary for its deacetylase activity. This binding leads to an increased level of acetylated histones, as the enzyme is no longer able to remove these functional groups effectively. Romidepsin operates through a similar mechanism but does so as a cyclic peptide that chelates the zinc ion within the active site of HDA4, which is vital for the enzyme's activity. Belinostat and Entinostat also inhibit HDA4 by binding to its active site, but they are notable for their selectivity, which allows for a more targeted approach in inhibiting the enzyme's function.
Chidamide is characterized by its benzamide structure, which interacts with the catalytic domain of HDA4, thereby inhibiting the enzyme. Similarly, Valproic Acid, a short-chain fatty acid, disrupts HDA4's catalytic activity, leading to an accumulation of acetylation on histonesChemical inhibitors of HDA4 impede its deacetylase function, which is essential for the regulation of chromatin structure and gene expression. Trichostatin A, for instance, inhibits HDA4 by preventing histone deacetylation, leading to a more open chromatin conformation. Vorinostat and Panobinostat are also inhibitors of HDA4, with the capability to bind to the enzyme's active site, thereby obstructing its function. These inhibitors result in the accumulation of acetylated histones, which can affect the expression of genes regulated by HDA4. Romidepsin, a cyclic peptide, operates through a mechanism of chelating the zinc ion in the active site of HDA4, essential for its deacetylase activity, which leads to the inhibition of the enzyme's function.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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 | $152.00 $479.00 $632.00 $1223.00 $2132.00 | 33 | |
Trichostatin A inhibits histone deacetylase (HDAC) activity, leading to an increase in acetylation of histones, which causes chromatin to become more open and less compact. Since HDA4 is a histone deacetylase, the increased acetylation directly counteracts its activity, thereby inhibiting its function. | ||||||
Suberoylanilide Hydroxamic Acid | 149647-78-9 | sc-220139 sc-220139A | 100 mg 500 mg | $133.00 $275.00 | 37 | |
Vorinostat is an HDAC inhibitor that binds to the active site of the enzyme, blocking its deacetylase activity. By inhibiting the deacetylation process, Vorinostat directly inhibits the function of HDA4 by preventing it from removing acetyl groups from histones. | ||||||
Panobinostat | 404950-80-7 | sc-208148 | 10 mg | $200.00 | 9 | |
Panobinostat is a potent HDAC inhibitor that binds to the zinc-containing active site of HDA4, leading to the accumulation of acetylated histones. This directly inhibits HDA4's ability to deacetylate histones, thereby inhibiting its enzymatic function. | ||||||
Romidepsin | 128517-07-7 | sc-364603 sc-364603A | 1 mg 5 mg | $218.00 $634.00 | 1 | |
Romidepsin is a cyclic peptide that inhibits HDACs by chelating the zinc ion in the active site of the enzyme. As a result, it directly inhibits HDA4 by blocking its ability to deacetylate histone proteins, leading to increased acetylation and transcriptional activation. | ||||||
Belinostat | 414864-00-9 | sc-269851 sc-269851A | 10 mg 100 mg | $156.00 $572.00 | ||
Belinostat is an HDAC inhibitor that directly inhibits the enzymatic activity of HDA4 by binding to its active site. This binding prevents HDA4 from removing acetyl groups from histone tails, which is its primary function. | ||||||
MS-275 | 209783-80-2 | sc-279455 sc-279455A sc-279455B | 1 mg 5 mg 25 mg | $24.00 $90.00 $212.00 | 24 | |
Entinostat selectively inhibits class I HDACs, which likely includes HDA4, by binding to the active site and preventing the enzyme from performing its deacetylation function on histone proteins. | ||||||
Chidamide | 743420-02-2 | sc-364462 sc-364462A sc-364462B | 1 mg 5 mg 25 mg | $62.00 $250.00 $1196.00 | ||
Chidamide is a benzamide HDAC inhibitor that interacts with the catalytic domain of HDACs, including HDA4, preventing the deacetylation of histones and thus inhibiting HDA4's enzymatic activity. | ||||||
Valproic Acid | 99-66-1 | sc-213144 | 10 g | $87.00 | 9 | |
Valproic Acid is a short-chain fatty acid and an HDAC inhibitor that inhibits HDA4 by disrupting the catalytic activity of the enzyme, leading to hyperacetylation of histones and inhibition of deacetylation. | ||||||
CI 994 | 112522-64-2 | sc-205245 sc-205245A | 10 mg 50 mg | $99.00 $536.00 | 1 | |
Tacedinaline is an HDAC inhibitor that competes with acetyl-lysine substrates for binding to the active site of HDA4, thereby inhibiting the deacetylation function of HDA4 on histone proteins. | ||||||
Mocetinostat | 726169-73-9 | sc-364539 sc-364539B sc-364539A | 5 mg 10 mg 50 mg | $214.00 $247.00 $1463.00 | 2 | |
Mocetinostat is an HDAC inhibitor that binds to the active site of HDA4, blocking its access to histone substrates and thus inhibiting its deacetylase activity, resulting in increased acetylation of histones. | ||||||