1.14.11.27: [histone-H3]-lysine-36 demethylase

This is an abbreviated version, for detailed information about [histone-H3]-lysine-36 demethylase, go to the full flat file.

Reaction

protein N6,N6-dimethyl-L-lysine
+
2-oxoglutarate
+
O2
=
protein N6-methyl-L-lysine
+
succinate
+
formaldehyde
+
CO2

Synonyms

AN1060, CG33182, CG33185, dJMJD2(1), dJMJD2(1)/CG15835, dJMJD2(2), dJMJD2(2)/CG33182, dKDM2, dKDM4A, dRAF, GASC1, Gis1, H3-K36 demethylase, H3-K36-specific demethylase, H3K36 demethylase, H3K36 histone demethylase, H3K36me2 demethylase, H3K36me2 histone demethylase, H3K36me2-specific demethylase, H3K9/36me3 lysine demethylase, H3K9/H3K36 histone demethylase, histone demethylase, histone demethylase JmjD2A, histone H3 demethylase, histone H3 lysine 36 demethylase, histone H3 lysine 36 dimethyl–specific demethylase, histone H3K36 demethylase, histone H3K9/H3K36 trimethyldemethylase, histone-lysine(H3-K36) demethylase, histoneH3 demethylase, Jhd1, JHDM1A, Jhdm1b/Kdm2b, JmjC demethylase, JmjC domain histone demethylase, JmjC domain lysine demethylase, JmjC domain-containing histone demethylase 1, JmjC domain-containing histone demethylase 1A, JmjC domain-containing histone demethylation protein 3A, JmjC domain-containing histone demethylation protein 3b, JmjC histone lysine demethylase, JmjC protein, JmjC+N, JmjC+N histone demethylase, JMJD2, Jmjd2 demethylase, JMJD2A, JMJD2B, JMJD2C, JMJD2D, JMJD5, JumonjiC demethylase, KDM2B, KDM2b/JHDM1b, KDM4, KDM4A, KDM4A demethylase, KDM4A/JMJD2A, KDM4B, Kdm4c, KDM4D, KDM8, KdmA, lysine demethylase, More, Ndy1, PfJmjC1, Rph1, Rph1/KDM4, scJHDM1, [histone-H3]-lysine-36 demethylase 1

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
                1.14.11.27 [histone-H3]-lysine-36 demethylase

Inhibitors

Inhibitors on EC 1.14.11.27 - [histone-H3]-lysine-36 demethylase

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INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-(2-((chroman-6-ylmethyl)amino)pyrimidin-4-yl)isonicotinic acid
-
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3-(9-(dimethylamino)-N-hydroxynonanamido)propanoic acid
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3-[hydroxy-[5-[[(1R)-2-(hydroxyamino)-2-oxo-1-[(4-phenylphenyl)methyl]ethyl]amino]-5-oxo-pentanoyl]amino]propanoic acid
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3-[hydroxy-[5-[[(1S)-2-(hydroxyamino)-2-oxo-1-[(4-phenylphenyl)methyl]ethyl]amino]-5-oxo-pentanoyl]amino]propanoic acid
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3-[hydroxy-[7-[[(1S)-2-methoxy-2-oxo-1-[(4-phenylphenyl)methyl]ethyl]amino]-7-oxo-heptanoyl]amino]propanoic acid
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3-[hydroxy-[8-[[(1R)-2-(hydroxyamino)-2-oxo-1-[(4-phenylphenyl)methyl]ethyl]amino]-8-oxo-octanoyl]amino]propanoic acid
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3-[hydroxy-[8-[[(1S)-2-(hydroxyamino)-2-oxo-1-[(4-phenylphenyl)methyl]ethyl]amino]-8-oxo-octanoyl]amino]propanoic acid
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3-[hydroxy-[8-[[(1S)-2-methoxy-2-oxo-1-[(4-phenylphenyl)methyl]ethyl]amino]-8-oxo-octanoyl]amino]propanoic acid
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5-tetrazolyl acetohydrazide
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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
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8-(hydroxyamino)-N-[(1S)-2-(hydroxyamino)-2-oxo-1-[(4-phenylphenyl)methyl]ethyl]-8-oxo-octanamide
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Co2+
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cobalt ions increase H3K9me3 and H3K36me3 by inhibiting histone demethylation process. Cobalt ions do not affect JMJD2A protein level but directly inhibit its demethylase activity. Exposure of both lung carcinoma A-549 cells and bronchial epithelial Beas-2B cells, to CoCl2 at 0.2 mM for 24 h increases methylation of histone H3 lysine residues 4, 9, 27 and 36, i.e. H3K4me3, H3K9me2, H3K9me3, H3K27me3, H3K36me3, as well as ubiquitination of histone H2A and H2B, while it decreases acetylation at histone H4, overview
methyl (2S)-2-[[4-[3-(hydroxyamino)-3-oxo-propyl]benzoyl]amino]-3-(4-phenylphenyl)propanoate
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methyl (2S)-2-[[7-(hydroxyamino)-7-oxo-heptanoyl]amino]-3-(4-phenylphenyl)propanoate
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methyl (2S)-2-[[7-[hydroxy-(3-methoxy-3-oxo-propyl)amino]-7-oxo-heptanoyl]amino]-3-(4-phenylphenyl)propanoate
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methyl (2S)-2-[[8-[hydroxy-(3-methoxy-3-oxo-propyl)amino]-8-oxo-octanoyl]amino]-3-(4-phenylphenyl)propanoate
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methyl (S)-3-(2’-chloro-6-hydroxy-[1,1'-biphenyl]-3-yl)-2-(8-(hydroxyamino)-8-oxooctanamido)propanoate
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methyl (S)-3-(3'-cyano-6-hydroxy-[1,1'-biphenyl]-3-yl)-2-(8-(hydroxyamino)-8-oxooctanamido)propanoate
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methyl (S)-3-(3'-fluoro-6-hydroxy-[1,1'-biphenyl]-3-yl)-2-(8-(hydroxyamino)-8-oxooctanamido)propanoate
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methyl (S)-3-(4'-chloro-6-hydroxy-[1,1'-biphenyl]-3-yl)-2-(8-(hydroxyamino)-8-oxooctanamido)propanoate
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methyl (S)-3-(4'-cyano-6-hydroxy-[1,1'-biphenyl]-3-yl)-2-(8-(hydroxyamino)-8-oxooctanamido)propanoate
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methyl (S)-3-(4'-fluoro-6-hydroxy-[1,1'-biphenyl]-3-yl)-2-(8-(hydroxyamino)-8-oxooctanamido)propanoate
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methyl (S)-3-(6-hydroxy-[1,1'-biphenyl]-3-yl)-2-(8-(hydroxyamino)-8-oxooctanamido)propanoate
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methyl (S)-3-([1,1'-biphenyl]-4-yl)-2-(8-(hydroxyamino)-8-oxooctanamido)propanoate
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methyl 3-(3'-chloro-6-hydroxy-[1,1'-biphenyl]-3-yl)-2-(8-(hydroxyamino)-8-oxooctanamido)propanoate
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methyl 3-[hydroxy-[8-[[(1S)-2-(hydroxyamino)-2-oxo-1-[(4-phenylphenyl)methyl]ethyl]amino]-8-oxo-octanoyl]amino]propanoate
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N-oxalylglycine
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i.e. NOG, a non-reactive 2-oxoglutarate analogue
N-[(1S)-2-(hydroxyamino)-2-oxo-1-[(4-phenylphenyl)methyl]ethyl]heptanamide
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N1-((3'-chloro-6-methoxy-[1,1'-biphenyl]-3-yl)methyl)-N8-hydroxyoctanediamide
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N1-(2-(3'-chloro-6-hydroxy-[1,1'-biphenyl]-3-yl)ethyl)-N8-hydroxyoctanediamide
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N1-(2-(3'-chloro-6-methoxy-[1,1'-biphenyl]-3-yl)ethyl)-N8-hydroxyoctanediamide
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Ni2+
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substitutes Fe2+ and inhibits the hydroxylation reaction
SW55
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a hydroxamate-based histone deacetylase (HDAC) inhibitor, slight inhibition
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tert-butyl (2S)-2-[[8-(hydroxyamino)-8-oxo-octanoyl]amino]-3-(4-phenylphenyl)propanoate
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tert-butyl (2S)-2-[[8-(hydroxyamino)-8-oxo-octanoyl]amino]-3-phenyl-propanoate
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additional information
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