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1.14.11.67: [histone H3]-trimethyl-L-lysine4 demethylase

This is an abbreviated version!
For detailed information about [histone H3]-trimethyl-L-lysine4 demethylase, go to the full flat file.

Word Map on EC 1.14.11.67

Reaction

a [histone H3]-N6,N6,N6-trimethyl-L-lysine4
+ 3 2-oxoglutarate + 3 O2 =
a [histone H3]-L-lysine4
 + 3 succinate + 3 formaldehyde + 3 CO2

Synonyms

amine oxidase (flavin-containing) domain 1, AOF1, At2g34880, CG33182, CG33185, CG3654, dJARID2, dJARID2/CG3654, dJMJD2(1), dJMJD2(1)/CG15835, dJMJD2(2), dJMJD2(2)/CG33182, Fbxl10, GH09982, H3K4 demethylase, H3K4 demethylase lysine-specific demethylase 5A, H3K4 histone demethylase, H3K4me3 demethylase, H3K4me3 histone demethylase, H3K4me3-specific demethylase, H3K4me3/2 histone demethylase, H3K9 trimethyl demethylase, histone 3 lysine 4 demethylase, histone demethylase, histone H3 lysine 4 demethylase, histone H3 lysine-4 demethylase, histone H3-K4 demethylase, histone H3K4 demethylase, histone H3K4-specific demethylase, histone lysine demethylase, histone-H3K4-specific demethylase, Jarid1, Jarid1a, JARID1B, JARID1C, Jarid2, JaridB, Jhd2, Jhdm1b/Kdm2b, JMJ15, JMJ703, JmjC domain histone demethylase, JmjC domain-containing histone demethylation protein 3A, JmjC domain-containing histone demethylation protein 3b, JmjC+N, JmjC+N histone demethylase, JMJD2A, JMJD2A-tudor, JMJD2B, jumonji AT rich interactive domain 1B, jumonji AT-rich interactive domain 1B, Jumonji demethylase, KDM1, KDM1B, KDM2, KDM5, KDM5A, KDM5B, KDM5b/JARID1b, KDM5C, KDM5D, Lid, little imaginal discs, LSD1, lysine demethylase, lysine demethylase 5b, lysine demethylase 7, lysine-specific demethylase, lysine-specific demethylase 1, lysine-specific demethylase 5A, lysine-specific demethylase 5B, lysine-specific demethylase JMJ703, Lysine-specific demethylase SE14, More, Ndy1, Os03g0151300, PHD finger protein 8, PHF8, PKDM7B, PLU-1, PLU1, RB-binding protein 2, RBP2, RBR-2, retinoblastoma binding protein 2, SE14, SMCX, trimethylated lysine 4 of histone H3 demethylase

ECTree

     1 Oxidoreductases
         1.14 Acting on paired donors, with incorporation or reduction of molecular oxygen
             1.14.11 With 2-oxoglutarate as one donor, and incorporation of one atom of oxygen into each donor
                1.14.11.67 [histone H3]-trimethyl-L-lysine4 demethylase

Inhibitors

Inhibitors on EC 1.14.11.67 - [histone H3]-trimethyl-L-lysine4 demethylase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(3-phenyl-1-(p-tolyl)-1H-pyrazol-4-yl)(4-(2-(pyrrolidin-1-yl) ethyl)piperazin-1-yl) methanone
-
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(E)-2-((3-(4-(dimethylamino)but-2-enamido)-phenyl)(2-(piperidin-1-yl)ethoxy)methyl)thieno[3,2-b]pyridine-7-carboxylic acid
-
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(R)-2-(1-(1-benzoylpiperidin-3-yl)-1H-1,2,3-triazol-4-yl)isonicotinic acid
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1-(2-methoxyphenyl)-N-(2-methyl-2-morpholinopropyl)-3-phenyl-1H-pyrazole-4-carboxamide
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1-(3-(ethylsulfonyl)phenyl)-2-(4-(pyridin-2-yl)thiazol-2-yl)ethan-1-one
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1-(3-(methylsulfonyl)phenyl)-2-(4-(pyridin-2-yl)thiazol-2-yl)ethan-1-one
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1-(4-(methylsulfonyl)phenyl)-2-(4-(pyridin-2-yl)thiazol-2-yl)ethan-1-one
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1-(4-methoxyphenyl)-N-(2-methyl-2-morpholinopropyl)-3-phenyl-1H-pyrazole-4-carboxamide
compound is a cellular active KDM5B inhibitor that can inhibit MKN45 cell proliferation, wound healing and migration. The compound can bind and stabilize KDM5B and induce the accumulation of H3K4me2/3
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1-phenyl-2-(4-(pyridin-2-yl)thiazol-2-yl)ethan-1-one
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2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)-N-ethylisonicotinamide
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2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)-N-methylisonicotinamide
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2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinamide
the potent and selective KDM5A-D inhibitor stops cellular demethylation of H3K4me3 at transcription start sites and proliferation of MM1S myeloma cells; the potent and selective KDM5A-D inhibitor stops cellular demethylation of H3K4me3 at transcription start sites and proliferation of MM1S myeloma cells; the potent and selective KDM5A-D inhibitor stops cellular demethylation of H3K4me3 at transcription start sites and proliferation of MM1S myeloma cells. Analysis of enzyme-inhibitor binding structure from crystal structure analysis, overview
2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinic acid
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2-((2-chlorophenyl)(2-(1-methylpyrrolidin-2-yl)-ethoxy)methyl)thieno[3,2-b]pyridine-7-carboxylic acid
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2-((3-aminophenyl)(2-(piperidin-1-yl)ethoxy)methyl)thieno[3,2-b]-pyridine-7-carboxylic acid
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2-oxoglutarate-competitive inhibition
2-(1-hydroxyvinyl)isonicotinic acid
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2-(2-aminothiazol-4-yl)isonicotinamide
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2-(2-aminothiazol-4-yl)isonicotinic acid
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2-(2-benzamidothiazol-4-yl)isonicotinic acid
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2-(2-methylthiazol-4-yl)isonicotinic acid
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2-(piperazin-1-ylmethyl)isonicotinic acid
the potent and selective KDM5A-D inhibitor stops cellular demethylation of H3K4me3 at transcription start sites and proliferation of MM1S myeloma cells
2-(thiazol-4-yl)isonicotinic acid
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3-((2-(pyridin-2-yl)-6-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)pyrimidin-4-yl)amino)propanoic acid
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3-((2-(pyridin-2-yl)-6-(4-(vinylsulfonyl)-1,4-diazepan-1-yl)pyrimidin-4-yl)amino)propanoic acid
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3-((6-(4-acryloyl-1,4-diazepan-1-yl)-2-(pyridin-2-yl)-pyrimidin-4-yl)amino)propanoic acid
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3-(2-((2-aminoethyl)carbamoyl)pyridin-4-yl)benzoic acid
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3-(methylsulfonyl)-N-(4-(pyridin-3-yl)thiazol-2-yl)benzamide
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4-((methyl((1-(4-oxo-3,4-dihydropyrido[3,4-d]pyrimidin-8-yl)-1H-pyrazol-4-yl)methyl)amino)methyl)benzonitrile
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4-((methyl(2-(1-(4-oxo-3,4-dihydropyrido[3,4-d]pyrimidin-8-yl)-1H-pyrazol-4-yl)ethyl)amino)methyl)benzonitrile
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4-(1-(2-(1-(4-oxo-3,4-dihydropyrido[3,4-d]pyrimidin-8-yl)-1H-pyrazol-4-yl)ethyl)piperidin-4-yl)benzonitrile
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4-(methylsulfonyl)-N-(4-(pyridin-3-yl)thiazol-2-yl)benzamide
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4-(pyridin-3-yl)thiazol-2-amine
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8-(((furan-2-ylmethyl)amino)methyl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-((4-(pyridin-2-yl)piperazin-1-yl)methyl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-((4-methylpiperazin-1-yl)methyl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-((4-phenylpiperazin-1-yl)methyl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-((benzylamino)methyl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-((dimethylamino)methyl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(1-methyl-1H-pyrazol-3-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(1H-pyrazol-3-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(2-aminothiazol-4-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(((3,4-dichlorobenzyl)(methyl)amino)methyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-((dimethylamino)methyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-((methyl(4-(methylsulfonyl)benzyl)amino)methyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-((4-fluorobenzyl) (methyl)amino)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-((5-cyclopropyl-1,2,4-oxadiazol-3-yl)methyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(2,4-difluorophenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(2-chlorophenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(3,4-dichlorobenzyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(3,5-dichlorophenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
substitution from C4 of the pyrazole moiety allows access to the histone peptide substrate binding site, incorporation of a conformationally constrained 4-phenylpiperidine linker gives derivatives such as 8-(4-(2-(4-(3-chlorophenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one which demonstrates equipotent activity versus the KDM4 (JMJD2) and KDM5 (JARID1) subfamily demethylases, selectivity over representative exemplars of the KDM2, KDM3, and KDM6 subfamilies, and cellular permeability in the Caco-2 assay
8-(4-(2-(4-(3,5-difluorophenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(3-(trifluoromethyl)phenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(3-chlorophenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
substitution from C4 of the pyrazole moiety allows access to the histone peptide substrate binding site, incorporation of a conformationally constrained 4-phenylpiperidine linker gives derivatives such as 8-(4-(2-(4-(3-chlorophenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one which demonstrates equipotent activity versus the KDM4 (JMJD2) and KDM5 (JARID1) subfamily demethylases, selectivity over representative exemplars of the KDM2, KDM3, and KDM6 subfamilies, cellular permeability in the Caco-2 assay, and inhibition of H3K9Me3 and H3K4Me3 demethylation in a cell-based assay
8-(4-(2-(4-(3-methoxybenzyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(4-(methylsulfonyl)phenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(4-(trifluoromethyl)benzyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(4-chlorobenzyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(4-chlorophenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(4-fluorobenzyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(4-fluorophenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(4-methoxyphenyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(benzo[d][1,3]dioxol-5-ylmethyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(pyridin-3-ylmethyl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(pyridin-4-yl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-(thiophen-2-yl)piperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-benzylpiperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(2-(4-phenylpiperidin-1-yl)ethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(hydroxymethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(piperidin-1-ylmethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(4-(pyrrolidin-1-ylmethyl)-1H-pyrazol-1-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(piperidin-1-ylmethyl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-(thiazol-4-yl)pyrido[3,4-d]pyrimidin-4(3H)-one
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8-chloropyrido[3,4-d]pyrimidin-4(3H)-one
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Cd2+
at 0.001-0.005 mM, cadmium increases global histone H3 methylation, H3K4me3 and H3K9me2, by inhibiting the activities of histone demethylases, and aberrant histone methylation that occurs early (48 h) and at 4 weeks is associated with cadmium-induced transformation of BEAS-2B cells at the early stage; at 0.001-0.005 mM, cadmium induces histone H3 lysine methylation by inhibiting histone demethylase activity on H3K4 and H3K9. Cadmium increases global histone H3 methylation, H3K4me3 and H3K9me2, by inhibiting the activities of histone demethylases, and aberrant histone methylation that occurs early (48 h) and at 4 weeks is associated with cadmium-induced transformation of BEAS-2B cells at the early stage
CPI-455
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EDTA
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ethyl 1-[3-[(4-methoxybenzene-1-sulfonyl)amino]benzoyl]prolinate
upon treatment with 30 microM, a strong increase of cells in G2/M and of the subG1 fraction is noted
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ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate
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ethyl 2-([(2-([2-(dimethylamino)ethyl](ethyl)amino)-2-oxoethyl)amino]methyl)pyridine-4-carboxylate
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KDM5-C70
ethyl 2-[3-[(4-methoxybenzene-1-sulfonyl)amino]benzoyl]benzoate
compound can selectively inhibit KDM5 enzymes and is capable of increasing sensitivity of breast cancer cells to ionizing radiation and radiation-induced damage. The compound does not show any significant effect on cell cycle
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GSK-J1
a selective inhibitor of the KDM6/KDM5 subfamilies. Docking study and identification of critical residues for binding of the inhibitor to the reconstituted KDM5 Jumonji domain; a selective inhibitor of the KDM6/KDM5 subfamilies. Docking study and identification of critical residues for binding of the inhibitor to the reconstituted KDM5 Jumonji domain. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5fold increased potency compared with that of KDM5B at 1 mM 2-oxoglutarate. Also inhibits the enzyme mutant KDM5BDELTAAP; a selective inhibitor of the KDM6/KDM5 subfamilies. Docking study and identification of critical residues for binding of the inhibitor to the reconstituted KDM5 Jumonji domain. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5fold increased potency compared with that of KDM5B at 1 mM 2-oxoglutarate. Also inhibits the enzyme mutant KDM5CDELTAAP
JIB 04
inhibitor is active against native and temozolomide-resistant glioblastoma cells. GSK J4, inhibitor of lysine demethylase KDM6B, EC 1.14.11.68, and JIB 04 strongly synergize and are a potent combination against temozolomide-resistant glioblastoma cells
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JIB-04
a pan-inhibitor of the Jumonji demethylase superfamily; a pan-inhibitor of the Jumonji demethylase superfamily, that is about 8fold more potent against KDM5B than against KDM5C. Also inhibits the enzyme mutant KDM5BDELTAAP; a pan-inhibitor of the Jumonji demethylase superfamily, that is about 8fold more potent against KDM5B than against KDM5C. Also inhibits the enzyme mutant KDM5CDELTAAP
K+
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strong inhibition at 50 mM
KDOAM-25
lithium 2-(((furan-2-ylmethyl)amino)methyl)isonicotinate
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lithium 2-((benzylamino)methyl)isonicotinate
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Mg2+
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75% inhibition at 50 mM
N-[2-(pyridin-2-yl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)pyrimidin-4-yl]-beta-alanine
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GSK-J1
NURF-1
an H3K4me3-binding protein and member of the chromatin-remodeling complex NURF, is required for promoting aberrant wsp-1 transcription in rbr-2 mutants and its ablation restores wild-type expression of wsp-1 and axon guidance
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Pargyline
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pyrido[3,4-d]pyrimidin-4(3H)-one
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tranylcypromine
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additional information
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