n-methyltransferase

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

Amodiaquine is a synthetic aminoquinoline, used to treat malaria.

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

Quinacrine dihydrochloride (Mepacrine dihydrochloride) is the dihydrochloride salt of the 9-aminoacridine derivative quinacrine with potential antineoplastic and antiparasitic activities.

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

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

Phenylethanolamine N-methyl transferase, bovine, is a biocatalyst and a pivotal enzyme in emerging biocatalyst technology. Enzyme engineering focuses on improving reaction kinetics, substrate selectivity, and activity in extreme conditions (e.g., low or high pH). Modifying these enzymes to introduce stimulus responsiveness also enables dynamic control of their activity.

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 belongs to small molecule inhibitors, serving as a nicotinamide N-methyltransferase (NNMT) inhibitor (IC50=33 nM (human), 190 nM (monkey), 210 nM (mouse)), with oral activity and cell permeability, for research on metabolic disorders, possessing insulin-sensitizing, glucose-lowering, and weight-reducing effects.

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.

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.

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

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.

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

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.

NNMT-IN-5 (Compound 3-12) is a potent inhibitor of nicotinamide N-methyltransferase (NNMT) with an IC50 value of 47.9 ± 0.6 nM. This compound exhibits exceptional selectivity for a set of human methyltransferases. NNMT-IN-5 is applicable in research related to cancer, diabetes, metabolic disorders, and neurodegenerative diseases.

Desmethylastemizole (O-Demethylastemizole) is a metabolite of Astemizole and acts as a β-hematin (βH) inhibitor. It exhibits antimalarial activity against Plasmodium falciparum strains Pf3D7, PfDd2, and PfItG with IC50 values of 0.12 μM, 0.11 μM, and 0.06 μM, respectively. Additionally, Desmethylastemizole functions as a histamine H1 receptor antagonist and significantly blocks the hERG K+ channel while inhibiting the activity of the histone-lysine N-methyltransferase EZH2. It is utilized in studies of long QT syndrome and malaria.