m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03150
 [1]
Histone modification H3K9me2 G9a METTL3 Direct Enhancement m6A modification CX3CR1 CX3CR1 METTL3 Methylation : m6A sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
 Regulator Info 
m6A Target CX3C chemokine receptor 1 (CX3CR1)
 Targert Gene 
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Histone modification (HistMod)
Epigenetic Regulator Histone-lysine N-methyltransferase EHMT2 (EHMT2) WRITER View Details
Regulated Target Histone H3 lysine 9 dimethylation (H3K9me2) View Details
Downstream Gene METTL3 View Details
Crosstalk Relationship Histone modification  →  m6A Enhancement
Crosstalk Mechanism histone modification directly impacts m6A modification through modulating the level of m6A regulator
Crosstalk Summary EHMT2 promotes m6A methyltransferase activity of METTL3, which upregulates PD-L1, CX3C chemokine receptor 1 (CX3CR1) and CASP1, at translational/post-translational level by regulating Histone H3 lysine 9 dimethylation (H3K9me2) level during ET.
Responsed Disease Inflammatory response ICD-11: MG46
 Disease Info 
In-vitro Model
 HEK293T Normal Homo sapiens CVCL_0063
RAW 264.7 Mouse leukemia Mus musculus CVCL_0493
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Histone-lysine N-methyltransferase EHMT2 (EHMT2) 7 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name MS012 Preclinical [2]
Synonyms
CHEMBL4086403; 2089617-83-2 (free base); N2-hexyl-6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine; BDBM50501525; N~2~-hexyl-6,7-dimethoxy-N~4~-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine
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MOA Inhibitor
External Link
CID: 137348638
TTD: DJ1Q9B
 Compound Name BIX-01294 Preclinical [3]
Synonyms
BIX01294; BIX 01294
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MOA Inhibitor
Activity IC50 = 67 nM
External Link
CID: 25150857
TTD: D06PPL
 Compound Name A-366 Preclinical [4]
Synonyms
A 366; A366
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MOA Inhibitor
Activity IC50 = 3 nM
External Link
CID: 76285486
TTD: D0C5EG
 Compound Name UNC0321 Investigative [5]
Synonyms
UNC-0321; UNC 0321
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MOA Inhibitor
Activity IC50 = 9000 nM
External Link
CID: 46901937
TTD: D0CX4W
 Compound Name BRD9539 Investigative [6]
Synonyms
BRD-9539; BRD 9539
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MOA Inhibitor
Activity IC50 = 1500 nM
External Link
CID: 73755260
TTD: D0RO9T
 Compound Name UNC0642 Investigative [7]
Synonyms
1481677-78-4; UNC 0642; UNC-0642; CHEMBL2441082; 2-(4,4-Difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine; Barrett; GTPL7017; SCHEMBL17372593; AOB2595; MolPort-035-765-953; EX-A2241; BCP08266; ZINC96285772; BDBM50442103; AKOS024458509; SB19046; CS-5269; NCGC00189140-01; NCGC00189140-02; AS-16721; HY-13980; BC600721; AK547424; UNC0642, > KB-146019; J-008448
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MOA Inhibitor
Activity IC50 < 2.5 nM
External Link
CID: 53315878
TTD: D0BI4T
 Compound Name UNC0638 Investigative [8]
Synonyms
1255580-76-7; UNC-0638; UNC 0638; UNII-26A103L2FO; 2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine; CHEMBL1231795; 26A103L2FO; 2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine; 1255517-77-1; 2-cyclohexyl-6-methoxy-N-[1-(propan-2-yl)piperidin-4-yl]-7-[3-(pyrrolidin-1-yl)propoxy]quinazolin-4-amine; 2-Cyclohexyl-N-(1-isopropyl-4-piperidinyl)-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
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MOA Inhibitor
Activity Ki = 3.7 nM
External Link
CID: 46224516
TTD: D0GK7A
References
Ref 1 Non-canonical function of histone methyltransferase G9a in the translational regulation of chronic inflammation. Cell Chem Biol. 2023 Dec 21;30(12):1525-1541.e7. doi: 10.1016/j.chembiol.2023.09.012. Epub 2023 Oct 19.
Ref 2 Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease. Nat Rev Drug Discov. 2021 Apr;20(4):265-286. doi: 10.1038/s41573-020-00108-x. Epub 2021 Jan 19.
Ref 3 Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81. doi: 10.1016/j.molcel.2007.01.017.
Ref 4 Discovery and development of potent and selective inhibitors of histone methyltransferase g9a. ACS Med Chem Lett. 2014 Jan 2;5(2):205-9. doi: 10.1021/ml400496h. eCollection 2014 Feb 13.
Ref 5 Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57. doi: 10.1021/jm100478y.
Ref 6 A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7. doi: 10.1021/cb300139y. Epub 2012 Apr 30.
Ref 7 Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-42. doi: 10.1021/jm401480r. Epub 2013 Oct 31.
Ref 8 A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74. doi: 10.1038/nchembio.599.