MacroH2A2 Inhibitors
Chemical inhibitors of MacroH2A2 operate through various mechanisms to disrupt its role in chromatin modification and gene regulation. Trichostatin A, Entinostat, and SAHA (Vorinostat) are histone deacetylase inhibitors that increase the acetylation level of histones. Enhanced acetylation can reduce MacroH2A2's ability to compact chromatin, thus inhibiting its gene-suppressing effects. Similarly, Anacardic Acid impedes histone acetyltransferase activities, which can lead to a chromatin state less conducive to MacroH2A2's binding and structural modification. BIX-01294 and UNC1999 target histone methylation patterns; BIX-01294 inhibits G9a histone methyltransferase, while UNC1999 inhibits EZH2, part of the PRC2 complex responsible for tri-methylation of histone H3 on lysine 27. These alterations can disrupt MacroH2A2's preference for certain methylation marks on chromatin, thereby inhibiting its function.
Other chemical inhibitors affect DNA interactions with MacroH2A2. Mithramycin A binds to G-C rich DNA sequences, which could prevent MacroH2A2 from binding to these regions and exerting its regulatory functions. Chloroquine intercalates into DNA, which can interfere with the MacroH2A2-DNA interaction. Etoposide, by stabilizing the DNA-topoisomerase II complex, alters the chromatin structure, potentially hindering MacroH2A2's binding. Ricinoleic Acid serves as an epigenetic modulator, changing the chromatin landscape in a way that could inhibit MacroH2A2's chromatin-organizing activities. RG108, a DNA methyltransferase inhibitor, alters DNA methylation status, which can influence MacroH2A2's associated functions with methylated genomic regions. C646, by inhibiting the histone acetyltransferase p300, can decrease histone acetylation levels, possibly reducing MacroH2A2 interaction with chromatin. Collectively, these chemicals disrupt the chromatin-modifying functions of MacroH2A2 through various pathways, highlighting the protein's sensitivity to changes in the epigenetic environment.
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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 is a histone deacetylase inhibitor that can inhibit the deacetylation of histones, including MacroH2A2. This inhibition can enhance the acetylation status of MacroH2A2, thereby reducing its ability to compact chromatin and suppress gene expression. | ||||||
Mithramycin A | 18378-89-7 | sc-200909 | 1 mg | $55.00 | 6 | |
Mithramycin A binds to G-C rich DNA sequences, potentially inhibiting the DNA binding ability of MacroH2A2, as MacroH2A2 has been shown to prefer such sequences. This binding can prevent MacroH2A2 from exerting its chromatin-modifying effects. | ||||||
Chloroquine | 54-05-7 | sc-507304 | 250 mg | $69.00 | 2 | |
Chloroquine is known to intercalate into DNA, which can disrupt the interaction between DNA and MacroH2A2, leading to the functional inhibition of its chromatin-organizing ability. | ||||||
Etoposide (VP-16) | 33419-42-0 | sc-3512B sc-3512 sc-3512A | 10 mg 100 mg 500 mg | $51.00 $231.00 $523.00 | 63 | |
Etoposide stabilizes the DNA-topoisomerase II complex, preventing the religation of DNA strands. This can hinder the binding of MacroH2A2 to the chromatin by altering the chromatin structure and accessibility. | ||||||
Ricinoleic Acid | 141-22-0 | sc-205489 sc-205489A sc-205489B | 100 mg 1 g 10 g | $43.00 $228.00 $1046.00 | ||
Ricinoleic Acid acts as an epigenetic modulator which could alter the chromatin structure, thereby inhibiting the histone variant MacroH2A2 from effectively binding and exerting its chromatin-modifying functions. | ||||||
Anacardic Acid | 16611-84-0 | sc-202463 sc-202463A | 5 mg 25 mg | $102.00 $204.00 | 13 | |
Anacardic Acid inhibits histone acetyltransferase activities, which could lead to a less acetylated chromatin state, indirectly inhibiting MacroH2A2's ability to incorporate into the chromatin and modify its structure. | ||||||
BIX01294 hydrochloride | 1392399-03-9 | sc-293525 sc-293525A sc-293525B | 1 mg 5 mg 25 mg | $37.00 $112.00 $408.00 | ||
BIX-01294 is an inhibitor of the G9a histone methyltransferase, leading to changes in histone methylation patterns that may antagonize the chromatin incorporation or function of MacroH2A2. | ||||||
UNC1999 | 1431612-23-5 | sc-475314 | 5 mg | $142.00 | 1 | |
UNC1999 inhibits EZH2, a component of the PRC2 complex, which is responsible for tri-methylation of histone H3 on lysine 27. By inhibiting this process, MacroH2A2's preference for H3K27me3-marked chromatin regions can be disrupted, leading to its functional inhibition. | ||||||
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 is a selective histone deacetylase inhibitor that can increase the acetylation level of histones, which can negatively impact MacroH2A2's ability to bind to the chromatin and fulfill its role in chromatin compaction and gene regulation. | ||||||
Suberoylanilide Hydroxamic Acid | 149647-78-9 | sc-220139 sc-220139A | 100 mg 500 mg | $133.00 $275.00 | 37 | |
SAHA is a histone deacetylase inhibitor that raises the level of histone acetylation, potentially disrupting MacroH2A2’s ability to bind to chromatin and regulate gene expression due to changes in chromatin structure. | ||||||