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2.1.1.319: type I protein arginine methyltransferase

This is an abbreviated version!
For detailed information about type I protein arginine methyltransferase, go to the full flat file.

Word Map on EC 2.1.1.319

Reaction

2 S-adenosyl-L-methionine +

[protein]-L-arginine
= 2 S-adenosyl-L-homocysteine +
[protein]-Nomega,Nomega-dimethyl-L-arginine

Synonyms

arginine methyltransferase 1, CARM1, coactivator-associated arginine methyltransferase 1, coactivator-associated arginine methyltransferase 1 variant 5, EC 2.1.1.124, EC 2.1.1.125, EC 2.1.1.126, EC 2.1.1.23, Eucgr.C03665.1, PRMT I, PRMT-1, PRMT1, PRMT10, PRMT2, PRMT3, PRMT4, PRMT6, PRMT8, protein arginine methyltransferase 1, protein arginine methyltransferase 2, protein arginine methyltransferase 4, protein arginine methyltransferase 6, protein arginine methyltransferase I, protein arginine N-methyltransferase 2, protein arginine N-methyltransferase I, RMT1, Tb927.1.4690, Tb927.5.3960, type I protein arginine methyltransferase

ECTree

     2 Transferases
         2.1 Transferring one-carbon groups
             2.1.1 Methyltransferases
                2.1.1.319 type I protein arginine methyltransferase

Inhibitors

Inhibitors on EC 2.1.1.319 - type I protein arginine methyltransferase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
14-benzoylacenaphtho[1',2':4,5]pyrido[2,1-b][1,3]benzothiazol-13-ium
cell membrane permeable inhibitor that effectively blocks proliferation of cancer cells including HELA, K562, and MCF7. Prediction of the binding mode of the inhibitors by molecular docking analysis indicates that the inhibitors competitively occupy the binding site of the substrate and destroy the protein-protein interactions between CARM1 and its substrates
2-[2-[(2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl]ethyl]guanidine
4-([6-[(2H-1,3-benzodioxol-5-yl)amino]-5-nitropyrimidin-4-yl]amino)benzene-1-carboximidamide
-
4-[(6-amino-5-nitropyrimidin-4-yl)amino]benzene-1-carboximidamide
-
4-[(6-anilino-5-nitropyrimidin-4-yl)amino]benzene-1-carboximidamide
0.05 mM, 9% inhibition
4-[[5-nitro-6-(4-sulfamoylanilino)pyrimidin-4-yl]amino]benzene-1-carboximidamide
0.05 mM, 28% inhibition
4-[[6-(4-aminoanilino)-5-nitropyrimidin-4-yl]amino]benzene-1-carboximidamide
0.05 mM, 28% inhibition
4-[[6-(4-carbamimidoylanilino)-5-nitropyrimidin-4-yl]amino]benzamide
-
4-[[6-(4-cyanoanilino)-5-nitropyrimidin-4-yl]amino]benzene-1-carboximidamide
-
4-[[6-(4-hydroxy-3,5-dimethoxyanilino)-5-nitropyrimidin-4-yl]amino]benzene-1-carboximidamide
0.05 mM, 44% inhibition
5'-([(3S)-3-amino-3-carboxypropyl]3-[[(pyridin-2-yl)amino]propyl]amino)-5'-deoxyadenosine
-
5'-([(3S)-3-amino-3-carboxypropyl]5-[[(iminiomethyl)amino]pentyl]amino)-5'-deoxyadenosine
-
5'-[(3-aminopropyl)[3-[(pyridin-2-yl)amino]propyl]amino]-5'-deoxyadenosine
-
5'-[(3-aminopropyl)[3-[(pyrimidin-2-yl)amino]propyl]amino]-5'-deoxyadenosine
-
5'-[(3-aminopropyl)[5-[(iminiomethyl)amino]pentyl]amino]-5'-deoxyadenosine
-
5'-[(3-[[amino(iminio)methyl]amino]propyl)(3-aminopropyl)amino]-5'-deoxyadenosine
-
5'-[(4-[[amino(iminio)methyl]amino]butyl)(3-aminopropyl)amino]-5'-deoxyadenosine
-
9-(ethoxycarbonyl)-1,4,8b,11,12,17a-hexahydrodibenzo[f,h]isoquinolino[2,1-b]isoquinolin-10-ium
cell membrane permeable inhibitor that effectively blocks proliferation of cancer cells including HELA, K562, and MCF7. Prediction of the binding mode of the inhibitors by molecular docking analysis indicates that the inhibitors competitively occupy the binding site of the substrate and destroy the protein-protein interactions between CARM1 and its substrates
Bay 11-7082
-
inhibits the protein arginine methyltransferase 1 (PRMT1) activity in vitro, and treatment of cells with the inhibitor causes the decline of the levels of protein asymmetric dimethylarginine catalyzed by PRMT1
Bay 11-7085
-
inhibits the protein arginine methyltransferase 1 (PRMT1) activity in vitro, and treatment of cells with the inhibitor causes the decline of the levels of protein asymmetric dimethylarginine catalyzed by PRMT1
Ca2+
weak inhibitor, 25% of the initial activity remains in the presence of 10 mM CaCl2
N,N'-dimethyl-N'-(1-(4-(2,2,2-trifluoroethoxy)phenyl)-1H-tetrazol-5-yl-methyl)ethylenediamine hydrochloride
-
N,N'-dimethyl-N'-(1-(4-isopropoxyphenyl)-1H-tetrazol-5-yl-methyl)ethylenediamine hydrochloride
non-competitive inhibition pattern with respect to either S-adenosyl-L-methionine or substrate arginine. Potent PRMT1 inhibitor, which can be used as lead compound for further drug discovery
N,N'-dimethyl-N'-(1-(4-trifluoromethoxyphenyl)-1H-tetrazol-5-yl-methyl)ethylenediamine hydrochloride
-
N-(1-(4-isopropoxyphenyl)-1H-tetrazol-5-yl-methyl)-N-methyl-ethylenediamine hydrochloride
-
N-(3-bromobenzyl)-1-(2-(methylamino)ethyl)piperidin-4-amine
potent and selective inhibitor of CARM1. It is around 20fold selective for CARM1 over PRMT6 and highly selective over PRMT1, PRMT3, PRMT8 as well as PRMT5 and PRMT7
N-aminoethyl-N'-(1-(4-isopropoxyphenyl)-1H-tetrazol-5-yl-methyl)-piperazinehydrochloride
-
N1-methyl-N1-([4-[3-(trifluoromethyl)phenyl]-1H-pyrrol-3-yl]methyl)ethane-1,2-diamine
-
N1-methyl-N1-([5-[3-(trifluoromethyl)phenyl]-2H-1,2,3-triazol-4-yl]methyl)ethane-1,2-diamine
the inhibitor is inactive against PRMT1, 3 and 4
-
N1-methyl-N1-[(4-[4-[(propan-2-yl)oxy]phenyl]-1H-pyrrol-3-yl)methyl]ethane-1,2-diamine
the inhibitor displays high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. The inhibitor potently decreases cellular levels of histone arginine asymmetric dimethylation. MS094, a close analog of MS023, is developed which is inactive in biochemical and cellular assays, as a negative control for chemical biology studies. MS023 and MS094 are useful chemical tools for investigating the role of type I PRMTs in health and disease; the inhibitor displays high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. The inhibitor potently decreases cellular levels of histone arginine asymmetric dimethylation. MS094, a close analog of MS023, is developed which is inactive in biochemical and cellular assays, as a negative control for chemical biology studies. MS023 and MS094 are useful chemical tools for investigating the role of type I PRMTs in health and disease; the inhibitor displays high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. The inhibitor potently decreases cellular levels of histone arginine asymmetric dimethylation. MS094, a close analog of MS023, is developed which is inactive in biochemical and cellular assays, as a negative control for chemical biology studies. MS023 and MS094 are useful chemical tools for investigating the role of type I PRMTs in health and disease; the inhibitor displays high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. The inhibitor potently decreases cellular levels of histone arginine asymmetric dimethylation. MS094, a close analog of MS023, is developed which is inactive in biochemical and cellular assays, as a negative control for chemical biology studies. MS023 and MS094 are useful chemical tools for investigating the role of type I PRMTs in health and disease
N2-[6-(4-carbamimidoylanilino)-5-nitropyrimidin-4-yl]glycinamide
0.05 mM, 49% inhibition
phenyl vinyl sulfonate
-
inhibits the protein arginine methyltransferase 1 (PRMT1) activity in vitro, and treatment of cells with the inhibitor causes the decline of the levels of protein asymmetric dimethylarginine catalyzed by PRMT1
phenyl vinyl sulfone
-
inhibits the protein arginine methyltransferase 1 (PRMT1) activity in vitro, and treatment of cells with the inhibitor causes the decline of the levels of protein asymmetric dimethylarginine catalyzed by PRMT1
S-adenosyl-L-homocysteine
S-adenosylhomocysteine
-
sinefungin
TC-E5003
selective inhibitor of PRMT1
tert-butyl (4-[[6-(4-carbamimidoylanilino)-5-nitropyrimidin-4-yl]amino]phenyl)carbamate
-
additional information
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