NSUN5B Inhibitors
NSUN5B inhibitors encompass a range of chemical compounds that target the methylation processes where NSUN5B is directly involved, leading to its functional inhibition. For instance, nucleoside analogs such as 5-azacytidine and decitabine incorporate into RNA and DNA, respectively, trapping NSUN5B in a covalent intermediate state or leading to the inhibition of DNA methyltransferases, which potentially reduces transcriptional activation of the NSUN5B gene. Similarly, zebularine and S-adenosylhomocysteine, the latter being a product inhibitor, can interfere with the methylation cycle by competing with natural substrates or by directly inhibiting methyltransferase activity, thereby hampering NSUN5B's ability to methylate RNA. Compounds like RG108 and procainamide act more indirectly, targeting the methylation of DNA at gene promoter regions, which could result in lowered expression of NSUN5B.
Moreover, inhibitors such as hydralazine and disulfiram exert their effects through demethylation of DNA or by forming complexes that can inhibit a variety of enzymesincluding methyltransferases, which might impede NSUN5B's methyltransferase function. The presence of excess cytidine triphosphate (CTP) may serve as a competitive inhibitor to NSUN5B's catalytic activity, by providing an abundance of substrate that could hinder the enzyme's ability to correctly methylate its RNA targets. Other molecules, like nicotinamide, influence the acetylation status of proteins that could interact with NSUN5B, indirectly modifying its activity. Furthermore, compounds that bind to DNA, such as mithramycin A, can prevent transcription factors from accessing the NSUN5B promoter, potentially leading to a decrease in NSUN5B expression.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
5-Azacytidine | 320-67-2 | sc-221003 | 500 mg | $280.00 | 4 | |
A nucleoside analog of cytidine that incorporates into RNA and DNA during replication and transcription. 5-azacytidine can trap NSUN5B in a covalent intermediate state, leading to the functional inhibition of NSUN5B-mediated RNA methylation. | ||||||
RG 108 | 48208-26-0 | sc-204235 sc-204235A | 10 mg 50 mg | $128.00 $505.00 | 2 | |
A non-nucleoside DNA methyltransferase inhibitor. RG108 may prevent the methylation of promoter regions of genes involved in the expression of NSUN5B, thus indirectly reducing NSUN5B's functional activity by decreasing its expression. | ||||||
Zebularine | 3690-10-6 | sc-203315 sc-203315A sc-203315B | 10 mg 25 mg 100 mg | $126.00 $278.00 $984.00 | 3 | |
A cytidine analog that gets incorporated into DNA and inhibits DNA methylation. Zebularine may lead to decreased methylation of the gene promoter regions, indirectly diminishing NSUN5B expression levels. | ||||||
5-Aza-2′-Deoxycytidine | 2353-33-5 | sc-202424 sc-202424A sc-202424B | 25 mg 100 mg 250 mg | $214.00 $316.00 $418.00 | 7 | |
Another nucleoside analog similar to 5-azacytidine, decitabine is incorporated into DNA and inhibits DNA methyltransferases, potentially reducing transcriptional activation of the NSUN5B gene. | ||||||
Homocysteine | 6027-13-0 | sc-507315 | 250 mg | $195.00 | ||
A product inhibitor of methyltransferase reactions, which can inhibit NSUN5B activity by competing with S-adenosylmethionine, the universal methyl donor for methylation reactions, thus hampering NSUN5B's methyltransferase activity. | ||||||
Hydralazine-15N4 Hydrochloride | 304-20-1 (unlabeled) | sc-490605 | 1 mg | $480.00 | ||
Known to demethylate DNA by inhibiting DNA methyltransferase, potentially leading to reduced expression of NSUN5B. | ||||||
Disulfiram | 97-77-8 | sc-205654 sc-205654A | 50 g 100 g | $52.00 $87.00 | 7 | |
An inhibitor of acetaldehyde dehydrogenase that may also interact with copper to form a complex capable of inhibiting various cellular enzymes, including methyltransferases, potentially impeding NSUN5B's methyltransferase activity. | ||||||
Nicotinamide | 98-92-0 | sc-208096 sc-208096A sc-208096B sc-208096C | 100 g 250 g 1 kg 5 kg | $43.00 $65.00 $200.00 $815.00 | 6 | |
A form of vitamin B3 that serves as an inhibitor of SIRT1, a deacetylase. While not directly inhibiting NSUN5B, nicotinamide may influence the acetylation status of proteins that interact with NSUN5B, thus indirectly affecting its function. | ||||||
Mithramycin A | 18378-89-7 | sc-200909 | 1 mg | $54.00 | 6 | |
that binds to G-C rich DNA sequences, potentially preventing transcription factors from binding to the NSUN5B promoter region and thus decreasing its expression. | ||||||
Histone Lysine Methyltransferase Inhibitor Inhibitor | 935693-62-2 free base | sc-202651 | 5 mg | $148.00 | 4 | |
A diazepin-quinazolin-amine derivative that inhibits G9a and GLP histone methyltransferases. Indirectly, BIX-01294 may alter chromatin states and gene expression profiles, including that of NSUN5B, thereby potentially reducing NSUN5B activity. | ||||||