n-methyltransferase

Amodiaquine is a synthetic aminoquinoline, used to treat malaria.

Bisubstrate inhibitor 78 is an inhibitor of nicotinamide N-methyltransferase (NNMT; IC50= 1.41 μM).1It binds the NNMT active site in the binding pockets for the NNMT substrates S-adenosyl-L-methionine (SAM) and nicotinamide . Bisubstrate inhibitor 78 is selective for NNMT over histone-lysine N-methytransferase NSD2 and protein arginine methyltransferase 1 (PRMT1; IC50s = >50 μM for both). It reduces levels of 1-methylnicotinamide in, and inhibits proliferation of, HSC-2 oral cancer cells when used at a concentration of 100 μM.This compound is unstable in powder form and other related salt forms are recommended.

JBSNF-000028 is an orally active and potent nicotinamide N-methyltransferase (NNMT) inhibitor with inhibitory effects on human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT) with IC50s of 0.033 μM, 0.19 μM, and 0.21 μM, respectively.JBSNF-000028 can drive insulin sensitization and weight loss. 000028 drives insulin sensitization, glucose regulation and weight loss and can be used to study metabolic disorders.

N-Acetyl-5-hydroxytryptamine (O-Demethylmelatonin) , also known as Normelatonin, is the immediate precursor of melatonin. It is produced from serotonin by the enzyme aralkylamine N-acetyltransferase and is converted to melatonin by acetylserotonin O-methyltransferase. It can potently activate TrkB receptor.

N-Methylsarcosine (Dimethylglycine) is used as an athletic performance enhancer and immunostimulant. It is also used in the treatment of autism, epilepsy and mitochondrial disease. It is also employed as a biomarker of protein degradation in chronic obstructive lung disease (COPD) patients. Further, it is used as a substrate to identify, differentiate and characterize amino acid methyltransferase. It plays an important role in the development of glycine-based ionic liquids and emulsifiers.

N-acetyl-L-methionine is nutritionally and metabolically equivalent to L-methionine. Methionine is a dietary indispensable amino acid required for normal growth and development of humans, other mammals, and avian species. In addition to being a substrate

JBSNF-000088 is an Nicotinamide N-methyltransferase (NNMT)inhibitor. It is used for the treatment of metabolic disorders.

2-Octanone inhibits fatty acid synthase in rats and exhibits weak inhibitory activity against phenylethanolamine N-methyltransferase, and is widely used in biochemical experiments and drug synthesis research.

1-Methyl-1,2,3,4-tetrahydroisoquinoline is an inhibitor of phenylethanolamine N-methyltransferase and can be used in biochemical experiments and drug synthesis.

BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.

RG108 (N-Phthalyl-L-tryptophan) is a DNA methyltransferase inhibitor with an IC50 of 115 nM.

AMI-1 is an effective and selective Histone Methyltransferase (HMT) inhibitor (IC50: 3.0 8.8 μM, for yeast Hmt1p, and human PRMT1).

Chlorpromazine Sulfone Hydrochloride is a metabolite of Chlorpromazine -- an anti-emetic and anti-psychotic agent. It may also be used as a potential N-methyltransferase inhibitor.

Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.

Amodiaquine dihydrochloride dihydrate (Amodiaquine hydrochloride) is the hydrochloride salt of amodiaquine, an orally active 4-aminoquinoline derivative with antimalarial and anti-inflammatory properties.

Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and GPCR signaling, and it can act as a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptor sites.

4-Chloropyridine acts as an inhibitor of Nicotinamide N-methyltransferase (NNMT). Serving as a substrate for NNMT, this compound enhances the electrophilicity at the C4 position through methylation of the pyridine nitrogen. This modification facilitates an aromatic nucleophilic substitution reaction with the non-catalytic cysteine (C159) in NNMT, ultimately leading to suicidal activity inhibition of the enzyme. 4-Chloropyridine is a promising candidate for the development of activity-based probes targeting NNMT functions.

NSC 641396 is a ribonucleotide reductase (RNR) inhibitor with an IC50 value of 1.2 μM. Additionally, it acts as an inhibitor of protein arginine N-methyltransferase 9 (PRMT9) and exhibits antitumor properties.

NNMT-IN-6 hydrochloride (compound 78) is a potent inhibitor of nicotinamide N-methyltransferase (NNMT), exhibiting an IC50 of 1.41 μM and a Kd of 5.6 μM. It effectively suppresses the proliferation of HSC-2 human oral cancer cell lines.

1-Methylnicotinamide is the active metabolite of nicotinamide, formed by nicotinamide N-methyltransferase. 1-Methylnicotinamide induces the secretion of nitric oxide by human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner. When administered at a dose of 30 mg/kg, it can increase the level of 6-keto-prostaglandin F1α in rat plasma and inhibit collagen-induced thrombosis at the same dose.

Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a member of the 4-aminoquinoline class, is an antimalarial agent that also acts as a potent oral histamine N-methyltransferase inhibitor with a K i value of 18.6 nM. Additionally, it functions as a Nurr1 agonist, targeting the Nurr1-LBD (ligand binding domain) with an EC 50 of approximately 20 μM, demonstrating anti-inflammatory effects [1] [2] [3] [4] [5].

LY 78335 (1-(2,3-Dichlorophenyl)ethanamine hydrochloride) is a phenylethanolamine-N-methyltransferase (PNMT) inhibitor.

histamine N-methyltransferase inhibitor

PDAT is a noncompetitive Indolethylamine N-methyltransferase inhibitor.