MacroH2A Activators
The MacroH2A Activators class is a collection of chemical compounds that can enhance the functional activity of MacroH2A, a variant of the histone H2A. MacroH2A plays a crucial role in chromatin structure and function, affecting gene expression byaltering chromatin compactness and accessibility. These activators operate through various mechanisms to enhance MacroH2A's function, primarily by modifying the balance of histone acetylation, a key process in chromatin structure regulation. In one approach, compounds such as NU7441 inhibit the function of DNA-PKcs, reducing the phosphorylation of MacroH2A and boosting its ability to compact chromatin. Others, like C646 and JQ1, target histone acetyltransferases and bromodomain proteins respectively, decreasing chromatin accessibility and thereby augmenting MacroH2A's gene repression role. A third group, including Vorinostat, MS-275, and Trichostatin A, inhibit histone deacetylases, raising histone acetylation levels, disrupting chromatin structure, and emphasizing MacroH2A's role in chromatin compaction.
An additional set of compounds, including Nicotinamide and Sirtinol, modulate sirtuin activity, affecting histone deacetylation and thereby impacting chromatin structure. This, in turn, enhances MacroH2A's ability to regulate gene expression through chromatin compaction. Finally, compounds like Curcumin exert influence by inhibiting specific cellular signaling pathways, which indirectly boosts MacroH2A's role in chromatin compaction and gene repression. Notably, all these activators, while diversely targeting various cellular processes, converge in their end effect of enhancing MacroH2A's function in chromatin structure regulation and gene expression control.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
NU 7441 | 503468-95-9 | sc-208107 | 5 mg | $357.00 | 10 | |
A potent DNA-PKcs inhibitor, NU 7441 enhances the activity of MacroH2A by reducing DNA repair processes. By inhibiting DNA-PKcs, it decreases the phosphorylation of MacroH2A, leading to an increase in its ability to compact chromatin and regulate gene expression. | ||||||
C646 | 328968-36-1 | sc-364452 sc-364452A | 10 mg 50 mg | $265.00 $944.00 | 5 | |
C646 is a competitive inhibitor of p300 and CBP histone acetyltransferases. By reducing the acetylation of histones, it decreases chromatin accessibility, leading to an enhanced role for MacroH2A in compacting chromatin and repressing gene transcription. | ||||||
(±)-JQ1 | 1268524-69-1 | sc-472932 sc-472932A | 5 mg 25 mg | $231.00 $863.00 | 1 | |
JQ1 is a potent inhibitor of the BET family of bromodomain proteins. By inhibiting these proteins, it reduces the reading of acetylated histones, thereby enhancing the role of MacroH2A in chromatin compaction and gene repression. | ||||||
Suberoylanilide Hydroxamic Acid | 149647-78-9 | sc-220139 sc-220139A | 100 mg 500 mg | $133.00 $275.00 | 37 | |
Suberoylanilide Hydroxamic Acid (SAHA) is a histone deacetylase (HDAC) inhibitor. By inhibiting HDAC, it increases histone acetylation and disrupts chromatin structure. This amplifies the role of MacroH2A in compacting chromatin and regulating gene expression. | ||||||
MS-275 | 209783-80-2 | sc-279455 sc-279455A sc-279455B | 1 mg 5 mg 25 mg | $24.00 $90.00 $212.00 | 24 | |
MS-275 (Entinostat) is a potent class I HDAC inhibitor. It increases histone acetylation and disrupts chromatin structure, enhancing the role of MacroH2A in compacting chromatin and repressing gene transcription. | ||||||
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 (TSA) is an HDAC inhibitor that increases histone acetylation and disrupts chromatin structure, which amplifies the role of MacroH2A in compacting chromatin and regulating gene expression. | ||||||
Nicotinamide | 98-92-0 | sc-208096 sc-208096A sc-208096B sc-208096C | 100 g 250 g 1 kg 5 kg | $44.00 $66.00 $204.00 $831.00 | 6 | |
Nicotinamide is a pan-sirtuin inhibitor that impairs the deacetylation of histones, disrupting chromatin structure and enhancing the role of MacroH2A in compacting chromatin and repressing gene transcription. | ||||||
Curcumin | 458-37-7 | sc-200509 sc-200509A sc-200509B sc-200509C sc-200509D sc-200509F sc-200509E | 1 g 5 g 25 g 100 g 250 g 1 kg 2.5 kg | $37.00 $69.00 $109.00 $218.00 $239.00 $879.00 $1968.00 | 47 | |
Curcumin is an inhibitor of NF-κB signaling and can enhance the role of MacroH2A in chromatin compaction and gene repression by reducing the transcriptional activity of many genes. | ||||||
Sirtinol | 410536-97-9 | sc-205976 sc-205976A | 1 mg 5 mg | $38.00 $113.00 | 14 | |
Sirtinol is a sirtuin inhibitor that impairs the deacetylation of histones, disrupting chromatin structure and enhancing the role of MacroH2A in compacting chromatin and repressing gene transcription. | ||||||