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Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT . Metoprine is an antifolate and antitumor agent .
Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
JBSNF-000028 hydrochloride is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 μM, 0.19 μM and 0.21 μM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 hydrochloride can be used for the research of metabolic disorders .
JBSNF-000028 is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 µM, 0.19 µM and 0.21 µM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 can be used for the research of metabolic disorders .
JBSNF-000028 TFA is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 μM, 0.19 μM and 0.21 μM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 TFA can be used for the research of metabolic disorders .
SKF 91488 (Homodimaprit) dihydrochloride is a potent and noncompetitive histamine N-methyltransferase inhibitor with a Ki value of 0.9 microM. SKF 91488 dihydrochloride inhibits the methylation of labeled histamine in mice .
1-(2,3-Dichlorophenyl)ethanamine hydrochloride is a phenylethanolamine N-methyltransferase (PNMT) inhibitor. 1-(2,3-Dichlorophenyl)ethanamine hydrochloride effectively reduces blood pressure of spontaneously hypertensive. 1-(2,3-Dichlorophenyl)ethanamine hydrochloride can be used for the research of blood pressure .
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
NNMT-IN-3 (compound 14) is a potent and selective nicotinamide N-methyltransferaseNNMT inhibitor with IC50 values of 1.1 nM and 0.4 μM in cell-free and cell-based assays, respectively. NNMT-IN-3 can be used to research obesity, type 2 diabetes, alcohol-related liver disease, cancer, sarcopenia and so on .
NNMT-IN-5 (Compound 3-12) is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50 = 47.9 ± 0.6 nM). NNMT-IN-5 also has an excellent selectivity profile over a panel of human methyltransferases. NNMT-IN-5 can be used for the research of cancer, diabetes, metabolic disorders, and neurodegenerative diseases .
AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding .
AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding .
Amodiaquine-d10 is the deuterium labeled Amodiaquine. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect[1][2][3][4].
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (compound 11), a tetrahydroisoquinoline (THIQ) derivative, is a selective phenylethanolamine N-methyltransferase (PNMT) inhibitor with a Ki value of 0.3 μM. 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline can be used in research on psychiatric disorders related to Alzheimer's disease and Parkinson's disease .
NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .
JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent and orally active Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease .
NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50=1.2 μM) and selectively binds to the NNMT substrate-binding site residues . NNMTi promotes myoblast differentiation in vitro and enhances fusion and regenerative capacity of muscle stem cells (muSCs) in aged mice .
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying .
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying .
SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying .
N-(2-Carbamoyl-ethyl)-Val-Leu-anilide is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying .
SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (compound 11), a tetrahydroisoquinoline (THIQ) derivative, is a selective phenylethanolamine N-methyltransferase (PNMT) inhibitor with a Ki value of 0.3 μM. 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline can be used in research on psychiatric disorders related to Alzheimer's disease and Parkinson's disease .
The nicotinamide N-methyltransferase (NNMT) protein catalyzes the methylation of nicotinamide using S-adenosyl-L-methionine to form N1-methylnicotinamide. NNMT affects pluripotent embryonic stem cell development and acts as a metabolic regulator, affecting adipose tissue energy expenditure, gluconeogenesis, and cholesterol biosynthesis. Nicotinamide N-Methyltransferase/NNMT Protein, Human (His) is the recombinant human-derived Nicotinamide N-Methyltransferase/NNMT protein, expressed by E. coli , with C-His labeled tag. The total length of Nicotinamide N-Methyltransferase/NNMT Protein, Human (His) is 264 a.a., with molecular weight of ~25-30 kDa.
The HNMT protein plays a pivotal role in histamine metabolism, facilitating its inactivation through N-methylation. This enzymatic activity is crucial for histamine degradation, emphasizing HNMT's essential function in modulating histamine levels. Its involvement in regulating the airway response to histamine underscores its significance in maintaining physiological homeostasis, potentially impacting immune and inflammatory responses. HNMT Protein, Human (His) is the recombinant human-derived HNMT protein, expressed by E. coli , with N-His labeled tag. The total length of HNMT Protein, Human (His) is 292 a.a., with molecular weight of ~32 kDa.
The nicotinamide N-methyltransferase (NNMT) protein catalyzes the methylation of nicotinamide using S-adenosyl-L-methionine to form N1-methylnicotinamide. NNMT affects pluripotent embryonic stem cell development and acts as a metabolic regulator, affecting adipose tissue energy expenditure, gluconeogenesis, and cholesterol biosynthesis. NNMT Protein, Human (GST) is the recombinant human-derived NNMT protein, expressed by E. coli , with N-GST labeled tag. The total length of NNMT Protein, Human (GST) is 264 a.a., with molecular weight of 56.6 kDa.
Glycine N-methyltransferase (GNMT) is responsible for catalyzing the methylation of glycine, using S-adenosylmethionine (AdoMet) to generate N-methylglycine (sarcosine), and simultaneously producing S-adenosyl homocysteine AdoHcy. This reaction is complexly regulated by 5-methyltetrahydrofolate binding, highlighting the critical role of GNMT in the regulation of methyl metabolism. GNMT Protein, Human (His) is the recombinant human-derived GNMT protein, expressed by E. coli , with N-6*His labeled tag. The total length of GNMT Protein, Human (His) is 295 a.a., with molecular weight of 31 & 80 kDa, respectively.
SMYD3 Protein, a histone methyltransferase, specifically induces di- and tri-methylation of H3K4, avoiding monomethylation, and methylates H4K5. Crucial in transcriptional activation within an RNA polymerase complex, SMYD3 also exhibits DNA-binding affinity for sequences containing 5'-CCCTCC-3' or 5'-GAGGGG-3'. Histone-lysine N-methyltransferase SMYD3 (SMYD3) Protein, Human (His-Myc) is the recombinant human-derived Histone-lysine N-methyltransferase SMYD3(SMYD3) protein, expressed by E. coli , with N-10*His, C-Myc labeled tag. Histone-lysine N-methyltransferase SMYD3 (SMYD3) Protein, Human (His-Myc), has molecular weight of 56.5 kDa.
Lysine methyltransferase (aKMT) is responsible for catalyzing the methylation of lysine residues in target proteins, using S-adenosyl-L-methionine (SAM) as a methyl donor. The enzyme exhibits broad substrate specificity, showing methylation primarily at "Lys-11", "Lys-16" and "Lys-31" of the vault chromatin protein Cren7 as well as several recombinant Sulfolobus proteins in vitro Ability. aKMT Protein, Sulfolobus islandicus is the recombinant aKMT protein, expressed by E. coli , with tag free. The total length of aKMT Protein, Sulfolobus islandicus is 160 a.a., .
GAMT protein uses S-adenosylmethionine as a methyl donor to catalyze the conversion of guanidinoacetic acid into creatine, playing a key role in cell metabolism. This enzyme activity is essential for the biosynthesis of creatine, a compound necessary for cellular energy storage and transport. GAMT Protein, Human (His) is the recombinant human-derived GAMT protein, expressed by E. coli , with N-6*His, C-6*His labeled tag. The total length of GAMT Protein, Human (His) is 236 a.a., with molecular weight of 27-32 kDa.
PRMT3 protein is a multifunctional protein arginine N-methyltransferase. As a type I methyltransferase, it catalyzes monomethylation and asymmetric dimethylation of arginine residues in target proteins. In addition to its methyltransferase role, PRMT3 may also regulate retinoic acid synthesis and signaling by inhibiting ALDH1A1 retinal dehydrogenase activity. PRMT3 Protein, Human (His) is the recombinant human-derived PRMT3 protein, expressed by E. coli , with N-10*His labeled tag. The total length of PRMT3 Protein, Human (His) is 530 a.a., with molecular weight of ~65 kDa.
KMT2D Protein, a histone methyltransferase, methylates histone H3 'Lys-4' (H3K4), predominantly establishing H3K4me1 marks at active chromatin sites. Integral to chromatin remodeling, it functions as a coactivator for the estrogen receptor, recruited by ESR1, activating transcription. KMT2D's role in depositing specific histone marks at genomic locations underscores its crucial involvement in modulating chromatin structure and gene expression. KMT2D Protein, Human is the recombinant human-derived KMT2D protein, expressed by E. coli , with tag free. The total length of KMT2D Protein, Human is 155 a.a., .
KMT2D Protein, a histone methyltransferase, methylates histone H3 'Lys-4' (H3K4), predominantly establishing H3K4me1 marks at active chromatin sites. Integral to chromatin remodeling, it functions as a coactivator for the estrogen receptor, recruited by ESR1, activating transcription. KMT2D's role in depositing specific histone marks at genomic locations underscores its crucial involvement in modulating chromatin structure and gene expression. KMT2D Protein, Human (GST) is the recombinant human-derived KMT2D protein, expressed by E. coli , with N-GST labeled tag. The total length of KMT2D Protein, Human (GST) is 155 a.a., .
Lysine methyltransferase (aKMT) is responsible for catalyzing the methylation of lysine residues in target proteins, using S-adenosyl-L-methionine (SAM) as a methyl donor. The enzyme exhibits broad substrate specificity, showing methylation primarily at "Lys-11", "Lys-16" and "Lys-31" of the vault chromatin protein Cren7 as well as several recombinant Sulfolobus proteins in vitro Ability. aKMT Protein, Sulfolobus islandicus (His, Strep) is the recombinant aKMT protein, expressed by E. coli , with N-Strep, N-6*His labeled tag. The total length of aKMT Protein, Sulfolobus islandicus (His, Strep) is 160 a.a., .
PRMT6, a versatile arginine methyltransferase, prefers asymmetrical dimethylarginine (aDMA) formation and methylates arginine residues within a glycine and arginine-rich domain. It orchestrates asymmetric dimethylation of histone H3 'Arg-2,' leading to H3R2me2a, a unique epigenetic tag associated with transcriptional repression. PRMT6 serves as a transcriptional repressor for various genes, including HOXA2, THBS1, and TP53, inhibiting cellular senescence by repressing TP53. It also methylates histones H2A and H4 'Arg-3,' acts as a coactivator for steroid hormone receptors, regulates alternative splicing, and plays a role in innate immunity against HIV-1. PRMT6 Protein, Human (HEK293, His-Flag) is the recombinant human-derived PRMT6 protein, expressed by HEK293, with N-Flag, C-His labeled tag. The total length of PRMT6 Protein, Human (HEK293, His-Flag) is 375 a.a., with molecular weight of 43-46 kDa.
SMYD3 Protein, a histone methyltransferase, specifically induces di- and tri-methylation of H3K4, avoiding monomethylation, and methylates H4K5. Crucial in transcriptional activation within an RNA polymerase complex, SMYD3 also exhibits DNA-binding affinity for sequences containing 5'-CCCTCC-3' or 5'-GAGGGG-3'. SMYD3 Protein, Human (sf9, GST) is the recombinant human-derived SMYD3 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of SMYD3 Protein, Human (sf9, GST) is 335 a.a., with molecular weight of ~58 kDa.
SUV420H2 protein is a histone methyltransferase that methylates H4K20 to generate H4K20me3 and H4K20me2, which are critical for transcriptional regulation and genome integrity. SUV420H2 functions in pericentric heterochromatin, establishes constitutive heterochromatin, and interacts with RB1 family proteins. SUV420H2 Protein, Human (His) is the recombinant human-derived SUV420H2 protein, expressed by E. coli , with N-His labeled tag. The total length of SUV420H2 Protein, Human (His) is 279 a.a., with molecular weight of ~60 kDa.
SMYD3 Protein, a histone methyltransferase, specifically induces di- and tri-methylation of H3K4, avoiding monomethylation, and methylates H4K5. Crucial in transcriptional activation within an RNA polymerase complex, SMYD3 also exhibits DNA-binding affinity for sequences containing 5'-CCCTCC-3' or 5'-GAGGGG-3'. SMYD3 Protein, Human (HEK293, His-Flag) is the recombinant human-derived SMYD3 protein, expressed by HEK293 , with C-His, C-Flag labeled tag. The total length of SMYD3 Protein, Human (HEK293, His-Flag) is 428 a.a., with molecular weight of ~49 kDa.
Contrary to the expected interaction, HEMK2 protein did not bind to TRMT112. This unique feature distinguishes HEMK2 from expected protein-protein interactions typically associated with its functional counterparts. HEMK2 Protein, Human (His) is the recombinant human-derived HEMK2 protein, expressed by E. coli , with C-His labeled tag. The total length of HEMK2 Protein, Human (His) is 186 a.a., with molecular weight of ~23 kDa.
The METTL11A protein methylates the N-terminus of target proteins, specifically catalyzing monomethylation, dimethylation, or trimethylation of exposed α-amino groups in the [Ala/Gly/Ser]-Pro-Lys motif. METTL11A Protein, Human is the recombinant human-derived METTL11A protein, expressed by E. coli , with tag free. The total length of METTL11A Protein, Human is 222 a.a., with molecular weight of ~25.5 kDa.
The METTL11A protein methylates the N-terminus of target proteins, specifically catalyzing monomethylation, dimethylation, or trimethylation of exposed α-amino groups in the [Ala/Gly/Ser]-Pro-Lys motif. METTL11A Protein, Human (GST) is the recombinant human-derived METTL11A protein, expressed by E. coli , with N-GST labeled tag. The total length of METTL11A Protein, Human (GST) is 222 a.a., with molecular weight of ~52.2 kDa.
The SMYD2 protein is a multifunctional methyltransferase that can modify histones and non-histone proteins, including p53/TP53 and RB1. Notably, it trimethylates H3 at "Lys-4" (H3K4me3), which is critical for gene activation. SMYD2 Protein, Human (sf9, His) is the recombinant human-derived SMYD2 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of SMYD2 Protein, Human (sf9, His) is 433 a.a., with molecular weight of ~48 kDa.
The SETD7 protein is a histone methyltransferase that specifically monomethylates H3K4, a mark associated with transcriptional activation. Its role in gene activation extends to the collagenase and insulin genes, specifically at the insulin promoter when IPF1/PDX-1 is recruited. SETD7 Protein, Human (His) is the recombinant human-derived SETD7 protein, expressed by E. coli , with N-His labeled tag. The total length of SETD7 Protein, Human (His) is 365 a.a., with molecular weight of 47-50 kDa.
Amodiaquine-d10 is the deuterium labeled Amodiaquine. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect[1][2][3][4].
![Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-<em>methyl</em>-pentanoyl]-Leu-Gly-OEt](http://file.medchemexpress.com/product_pic/hy-p4521.gif)
