PLAG1 Inhibitors
Chemical inhibitors of PLAG1 can exert their effects through various molecular mechanisms that interfere with the protein's activity. C646, for example, is a selective inhibitor of the enzyme p300, which is responsible for the acetylation of PLAG1 that activates it. By preventing this acetylation, C646 effectively reduces PLAG1's activity. Similarly, garcinol and anacardic acid target the same p300 enzyme, thereby diminishing PLAG1's functional activity via a lack of acetylation. Curcumin also inhibits histone acetyltransferases, resulting in a decrease of PLAG1 acetylation and subsequent activity. These inhibitors essentially prevent PLAG1 from undergoing post-translational modifications that are necessary for its full transcriptional activity.
In addition to these acetylation-focused inhibitors, there are compounds that affect PLAG1 activity through other modifications. BIX-01294 targets histone methyltransferase, potentially changing the methylation status of histones at PLAG1 target genes and thus impeding PLAG1's ability to effectively promote gene expression. MG-149 inhibits the histone acetyltransferase TIP60, which may work in tandem with PLAG1, so its inhibition can reduce PLAG1's transcriptional activation. Chloroquine disrupts the cellular environment, particularly lysosomal functions, which can indirectly lead to an accumulation of non-functional PLAG1 due to improper folding or modification. PD0325901 and quercetin inhibit kinases within the MAPK/ERK pathway and other kinase pathways, respectively, which are involved in PLAG1 phosphorylation and activation, reducing the protein's activity. Sinefungin interferes with methylation processes that could alter PLAG1's function, while triptolide can inhibit the transcriptional activities of nuclear factors including PLAG1. Lastly, I-CBP112 specifically inhibits the CBP/p300 bromodomains, which are crucial for PLAG1 activation, therefore directly decreasing PLAG1's transcriptional activity.
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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 acetylates PLAG1, leading to its activation. By inhibiting p300, C646 prevents the acetylation and subsequent activation of PLAG1, thereby reducing its functional activity in the cell. | ||||||
Garcinol | 78824-30-3 | sc-200891 sc-200891A | 10 mg 50 mg | $136.00 $492.00 | 13 | |
Garcinol is known to inhibit histone acetyltransferases like p300. Since p300 mediates the acetylation and activation of PLAG1, inhibition by garcinol leads to decreased acetylation and reduced activity of PLAG1. | ||||||
Anacardic Acid | 16611-84-0 | sc-202463 sc-202463A | 5 mg 25 mg | $100.00 $200.00 | 13 | |
Anacardic Acid is another inhibitor of p300 and other histone acetyltransferases. By inhibiting these enzymes, it can decrease the acetylation and thereby the activity of PLAG1 within the nucleus. | ||||||
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 a compound that has been shown to inhibit histone acetyltransferases. It can decrease the acetylation of PLAG1, reducing its activity as a transcription factor. | ||||||
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, which can alter the methylation status of histones that associate with PLAG1 target genes, potentially leading to the inhibition of PLAG1 function by changing the chromatin structure and decreasing gene expression. | ||||||
Chloroquine | 54-05-7 | sc-507304 | 250 mg | $68.00 | 2 | |
Chloroquine is known to alkalinize lysosomes and inhibit lysosomal enzymes. By altering the cellular environment, it can impede the degradation pathway of PLAG1, potentially leading to the accumulation of non-functional PLAG1 due to improper folding or post-translational modification. | ||||||
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 known to inhibit a wide range of kinases. It may inhibit kinases responsible for the phosphorylation and subsequent activation of PLAG1, leading to a decrease in its transcriptional activity. | ||||||
Sinefungin | 58944-73-3 | sc-203263 sc-203263B sc-203263C sc-203263A | 1 mg 100 mg 1 g 10 mg | $266.00 $5100.00 $39576.00 $690.00 | 4 | |
Sinefungin is a universal inhibitor of S-adenosylmethionine-dependent methyltransferases and can interfere with methylation processes that modulate the activity of transcription factors such as PLAG1, thus inhibiting its function. | ||||||
Triptolide | 38748-32-2 | sc-200122 sc-200122A | 1 mg 5 mg | $88.00 $200.00 | 13 | |
Triptolide is a diterpene triepoxide that has been shown to inhibit the transcriptional activity of various nuclear factors. It may inhibit the transcriptional activity of PLAG1 by interfering with its DNA-binding or transactivation functions. | ||||||
I-CBP112 | 1640282-31-0 | sc-507494 | 25 mg | $400.00 | ||
I-CBP112 is an inhibitor of the CBP/p300 bromodomains. Since CBP/p300 interacts with PLAG1 for its acetylation and activation, inhibition by I-CBP112 would prevent PLAG1 activation, leading to decreased transcriptional activity. | ||||||