BAZ2B Inhibitors
Chemical inhibitors of BAZ2B function through various mechanisms to impede its role in chromatin remodeling and recognition of methylated or acetylated histones. C646 acts by selectively inhibiting p300, a histone acetyltransferase that can acetylate BAZ2B, thereby reducing its ability to bind to nucleosomes effectively. Similarly, Garcinol and Anacardic Acid target p300 and PCAF, another histone acetyltransferase, which when inhibited, results in decreased acetylation of BAZ2B, limiting its chromatin-remodeling activity. Curcumin disrupts BAZ2B function by inhibiting the HAT activity of p300, which is essential for the acetylation and subsequent activation of BAZ2B. This disruption leads to a decrease in BAZ2B's capability to modulate chromatin structure.
Inhibitors like BIX-01294 and UNC0638 target the methylation recognition capacity of BAZ2B. BIX-01294 inhibits G9a HMTase, which methylates histone residues that BAZ2B recognizes and binds. UNC0638 further hinders BAZ2B function by inhibiting G9a and GLP histone methyltransferases, reducing BAZ2B's interaction with chromatin due to a decreased substrate for binding. Chaetocin and 3-Deazaneplanocin A also reduce histone methylation, with Chaetocin inhibiting SUV39H1 and 3-Deazaneplanocin A targeting EZH2, which in both cases would lead to a diminished ability of BAZ2B to bind its target methylated histones. Entinostat, a class I HDAC inhibitor, increases histone acetylation, possibly interfering with BAZ2B's interaction with methylated histones. Quercetin inhibits kinases that are responsible for BAZ2B phosphorylation, which is necessary for its activity, thereby indirectly reducing its function. MG-132 prevents the proteasomal degradation of proteins, which could interfere with ubiquitin-dependent signaling necessary for BAZ2B's activity. Finally, I-CBP112 competes with BAZ2B for binding to acetylated lysines on histones due to its inhibition of the bromodomains of CBP/p300, impeding BAZ2B's chromatin binding and subsequent function.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
C646 | 328968-36-1 | sc-364452 sc-364452A | 10 mg 50 mg | $260.00 $925.00 | 5 | |
C646 is a selective inhibitor of p300, a histone acetyltransferase that can acetylate the BAZ2B protein. By inhibiting p300, C646 can prevent the acetylation of BAZ2B, thereby reducing its binding ability to nucleosomes and inhibiting its function. | ||||||
Garcinol | 78824-30-3 | sc-200891 sc-200891A | 10 mg 50 mg | $136.00 $492.00 | 13 | |
Garcinol inhibits p300 as well as PCAF, another histone acetyltransferase that could potentially acetylate BAZ2B. Inhibition of these acetyltransferases by garcinol would lead to decreased acetylation of BAZ2B, reducing its chromatin-remodeling activity. | ||||||
Anacardic Acid | 16611-84-0 | sc-202463 sc-202463A | 5 mg 25 mg | $100.00 $200.00 | 13 | |
Anacardic Acid is an inhibitor of histone acetyltransferase enzymes like p300. By inhibiting the acetylation process, it can indirectly prevent the functional activation of BAZ2B, which relies on acetylation for its full activity. | ||||||
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 | $36.00 $68.00 $107.00 $214.00 $234.00 $862.00 $1968.00 | 47 | |
Curcumin is known to inhibit the HAT activity of p300, and thus could prevent the acetylation and subsequent activation of BAZ2B, leading to functional inhibition of its chromatin remodeling capabilities. | ||||||
BIX01294 hydrochloride | 1392399-03-9 | sc-293525 sc-293525A sc-293525B | 1 mg 5 mg 25 mg | $36.00 $110.00 $400.00 | ||
BIX-01294 is a histone methyltransferase inhibitor, specifically inhibiting G9a HMTase. BAZ2B recognizes and binds to specific methylated histone residues; thus, inhibition of histone methylation by BIX-01294 would decrease BAZ2B’s ability to interact with chromatin. | ||||||
UNC0638 | 1255580-76-7 | sc-397012 | 10 mg | $315.00 | ||
UNC0638 is an inhibitor of G9a and GLP histone methyltransferases, which methylate histone H3. By inhibiting these enzymes, the substrate for BAZ2B recognition is reduced, thereby inhibiting BAZ2B’s chromatin-remodeling function. | ||||||
Chaetocin | 28097-03-2 | sc-200893 | 200 µg | $120.00 | 5 | |
Chaetocin is a specific inhibitor of the histone methyltransferase SUV39H1. Since BAZ2B interaction with chromatin is methylation-dependent, inhibiting SUV39H1 can indirectly reduce BAZ2B’s ability to bind methylated histones and thus inhibit its function. | ||||||
MS-275 | 209783-80-2 | sc-279455 sc-279455A sc-279455B | 1 mg 5 mg 25 mg | $24.00 $88.00 $208.00 | 24 | |
Entinostat is a class I histone deacetylase inhibitor. By increasing histone acetylation, it can interfere with BAZ2B’s recognition of methylated histone marks, as BAZ2B has bromodomains that could be competitively inhibited by hyperacetylated histones. | ||||||
Quercetin | 117-39-5 | sc-206089 sc-206089A sc-206089E sc-206089C sc-206089D sc-206089B | 100 mg 500 mg 100 g 250 g 1 kg 25 g | $11.00 $17.00 $108.00 $245.00 $918.00 $49.00 | 33 | |
Quercetin is a flavonoid that can inhibit the activity of several kinases that might phosphorylate BAZ2B, leading to a change in its activity. By inhibiting these kinases, quercetin could indirectly reduce BAZ2B’s activity by preventing its phosphorylation-dependent functions. | ||||||
MG-132 [Z-Leu- Leu-Leu-CHO] | 133407-82-6 | sc-201270 sc-201270A sc-201270B | 5 mg 25 mg 100 mg | $56.00 $260.00 $980.00 | 163 | |
MG-132 is a proteasome inhibitor that can lead to increased levels of ubiquitinated proteins. This might interfere with the ubiquitin-dependent signaling pathways that could be necessary for BAZ2B’s full activity, thereby functionally inhibiting BAZ2B. | ||||||