METTL25 Inhibitors
Chemical inhibitors of METTL25 can exert their effects through various mechanisms, which involve direct interaction with the active site or indirect modulation of substrate or cofactor availability. S-Adenosylmethionine, a methyl group donor, is critical for the activity of METTL25. Compounds such as S-Adenosylmethionine itself can bind to the enzyme's active site, acting as an inhibitor by preventing the transfer of methyl groups to its substrates. Meclofenamic acid, by virtue of its structural similarity to the adenosyl moiety of S-Adenosylmethionine, can compete with this methyl donor, obstructing its binding to METTL25 and thus inhibiting the enzyme's methylation activity. Additionally, 5'-Methylthioadenosine, a byproduct of methylation reactions, can also inhibit METTL25 by mimicking the natural substrate and binding to the active site, which blocks further methylation processes.
Some inhibitors exert their influence indirectly by affecting the availability of S-Adenosylmethionine. For instance, 3-Deazaadenosine can lead to an accumulation of S-adenosylhomocysteine, a strong inhibitor of SAM-dependent methyltransferases, by inhibiting S-adenosylhomocysteine hydrolase. This accumulation can compete with S-Adenosylmethionine for the active site on METTL25. Sinomenine can alter METTL25's conformation, potentially preventing it from properly binding to SAM or its substrate. Inhibitors like Decitabine, RG108, BIX-01294, Chaetocin, and EPZ004777, despite their primary targets being other enzymes, can influence the methylation cycle or the methylation landscape in a way that affects the availability of S-Adenosylmethionine or alters the recognition of substrates by METTL25. Lastly, Quercetin can bind to METTL25 and affect its function via competition with substrates or cofactors, or by inducing conformational changes that interfere with the enzyme's activity.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Ademetionine | 29908-03-0 | sc-278677 sc-278677A | 100 mg 1 g | $184.00 $668.00 | 2 | |
S-Adenosylmethionine (SAM) is a common cosubstrate involved in methyl group transfers. METTL25 is a methyltransferase, and SAM could act as an inhibitor by binding to the active site of METTL25, thereby preventing the transfer of methyl groups to its substrates. | ||||||
Meclofenamic Acid | 644-62-2 | sc-211780 | 5 mg | $402.00 | ||
Meclofenamic acid is a nonsteroidal anti-inflammatory drug that can inhibit various enzymes. It can inhibit METTL25 by competing with the methyl donor S-Adenosylmethionine (SAM), as it has a similar structure to the adenosyl moiety of SAM, potentially preventing SAM from binding to METTL25's active site. | ||||||
5-Aza-2′-Deoxycytidine | 2353-33-5 | sc-202424 sc-202424A sc-202424B | 25 mg 100 mg 250 mg | $218.00 $322.00 $426.00 | 7 | |
Decitabine is a cytidine analog that incorporates into DNA and traps DNA methyltransferases. While METTL25 is not a DNA methyltransferase, decitabine can indirectly hinder the methylation cycle in which METTL25 participates, by depleting the pool of SAM through trapping DNA methyltransferases, potentially reducing the availability of SAM for METTL25. | ||||||
RG 108 | 48208-26-0 | sc-204235 sc-204235A | 10 mg 50 mg | $131.00 $515.00 | 2 | |
RG108 is a non-nucleoside DNA methyltransferase inhibitor. By inhibiting DNA methyltransferases, RG108 can indirectly affect the methylation cycle and the availability of SAM, the methyl donor for METTL25, potentially leading to reduced methylation activity of METTL25 due to lower SAM levels. | ||||||
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 G9a and GLP methyltransferases, which share some mechanistic features with METTL25. By inhibiting related methyltransferases, BIX-01294 could influence the overall methylation landscape and indirectly reduce the activity of METTL25 by altering intracellular methylation patterns and SAM availability. | ||||||
Chaetocin | 28097-03-2 | sc-200893 | 200 µg | $126.00 | 5 | |
Chaetocin is a specific inhibitor of the histone methyltransferase SUV39H1. By inhibiting histone methyltransferases, chaetocin can alter the balance of methylation in the cell. This change could indirectly inhibit METTL25 by affecting the availability of SAM and the methylation signaling pathways that METTL25 is involved in. | ||||||
Epz004777 | 1338466-77-5 | sc-507560 | 100 mg | $575.00 | ||
EPZ004777 is a potent, selective DOT1L histone methyltransferase inhibitor. While it is specific to DOT1L, its action can lead to broader effects on the cellular methylation environment and possibly deplete SAM levels or alter substrate recognition, indirectly inhibiting METTL25 by reducing the availability of the methyl donor. | ||||||
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 $110.00 $250.00 $936.00 $50.00 | 33 | |
Quercetin is a flavonoid that has been shown to inhibit protein kinases and other enzymes. It can inhibit METTL25 by competing with substrates or cofactors for binding sites on the enzyme, or by altering the enzymatic activity through conformational changes upon binding to the enzyme at allosteric sites. | ||||||