General Information of the Protein
Protein ID
PT02598
Protein Name
DNA (cytosine-5)-methyltransferase 1
Secondarily
Protein Name
CXXC-type zinc finger protein 9
DNA methyltransferase HsaI
MCMT
Gene Name
DNMT1
Secondarily
Gene Name
AIM
CXXC9
DNMT
Sequence
MPARTAPARVPTLAVPAISLPDDVRRRLKDLERDSLTEKECVKEKLNLLHEFLQTEIKNQLCDLETKLRKEELSEEGYLAKVKSLLNKDLSLENGAHAYNREVNGRLENGNQARSEARRVGMADANSPPKPLSKPRTPRRSKSDGEAKPEPSPSPRITRKSTRQTTITSHFAKGPAKRKPQEESERAKSDESIKEEDKDQDEKRRRVTSRERVARPLPAEEPERAKSGTRTEKEEERDEKEEKRLRSQTKEPTPKQKLKEEPDREARAGVQADEDEDGDEKDEKKHRSQPKDLAAKRRPEEKEPEKVNPQISDEKDEDEKEEKRRKTTPKEPTEKKMARAKTVMNSKTHPPKCIQCGQYLDDPDLKYGQHPPDAVDEPQMLTNEKLSIFDANESGFESYEALPQHKLTCFSVYCKHGHLCPIDTGLIEKNIELFFSGSAKPIYDDDPSLEGGVNGKNLGPINEWWITGFDGGEKALIGFSTSFAEYILMDPSPEYAPIFGLMQEKIYISKIVVEFLQSNSDSTYEDLINKIETTVPPSGLNLNRFTEDSLLRHAQFVVEQVESYDEAGDSDEQPIFLTPCMRDLIKLAGVTLGQRRAQARRQTIRHSTREKDRGPTKATTTKLVYQIFDTFFAEQIEKDDREDKENAFKRRRCGVCEVCQQPECGKCKACKDMVKFGGSGRSKQACQERRCPNMAMKEADDDEEVDDNIPEMPSPKKMHQGKKKKQNKNRISWVGEAVKTDGKKSYYKKVCIDAETLEVGDCVSVIPDDSSKPLYLARVTALWEDSSNGQMFHAHWFCAGTDTVLGATSDPLELFLVDECEDMQLSYIHSKVKVIYKAPSENWAMEGGMDPESLLEGDDGKTYFYQLWYDQDYARFESPPKTQPTEDNKFKFCVSCARLAEMRQKEIPRVLEQLEDLDSRVLYYSATKNGILYRVGDGVYLPPEAFTFNIKLSSPVKRPRKEPVDEDLYPEHYRKYSDYIKGSNLDAPEPYRIGRIKEIFCPKKSNGRPNETDIKIRVNKFYRPENTHKSTPASYHADINLLYWSDEEAVVDFKAVQGRCTVEYGEDLPECVQVYSMGGPNRFYFLEAYNAKSKSFEDPPNHARSPGNKGKGKGKGKGKPKSQACEPSEPEIEIKLPKLRTLDVFSGCGGLSEGFHQAGISDTLWAIEMWDPAAQAFRLNNPGSTVFTEDCNILLKLVMAGETTNSRGQRLPQKGDVEMLCGGPPCQGFSGMNRFNSRTYSKFKNSLVVSFLSYCDYYRPRFFLLENVRNFVSFKRSMVLKLTLRCLVRMGYQCTFGVLQAGQYGVAQTRRRAIILAAAPGEKLPLFPEPLHVFAPRACQLSVVVDDKKFVSNITRLSSGPFRTITVRDTMSDLPEVRNGASALEISYNGEPQSWFQRQLRGAQYQPILRDHICKDMSALVAARMRHIPLAPGSDWRDLPNIEVRLSDGTMARKLRYTHHDRKNGRSSSGALRGVCSCVEAGKACDPAARQFNTLIPWCLPHTGNRHNHWAGLYGRLEWDGFFSTTVTNPEPMGKQGRVLHPEQHRVVSVRECARSQGFPDTYRLFGNILDKHRQVGNAVPPPLAKAIGLEIKLCMLAKARESASAKIKEEEAAKD
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Writer
>
DNA methyltransferase
Function
Methylates CpG residues. Preferentially methylates hemimethylated DNA. Associates with DNA replication sites in S phase maintaining the methylation pattern in the newly synthesized strand, that is essential for epigenetic inheritance. Associates with chromatin during G2 and M phases to maintain DNA methylation independently of replication. It is responsible for maintaining methylation patterns established in development. DNA methylation is coordinated with methylation of histones. Mediates transcriptional repression by direct binding to HDAC2. In association with DNMT3B and via the recruitment of CTCFL/BORIS, involved in activation of BAG1 gene expression by modulating dimethylation of promoter histone H3 at H3K4 and H3K9. Probably forms a corepressor complex required for activated KRAS-mediated promoter hypermethylation and transcriptional silencing of tumor suppressor genes (TSGs) or other tumor-related genes in colorectal cancer (CRC) cells (PubMed:24623306). Also required to maintain a transcriptionally repressive state of genes in undifferentiated embryonic stem cells (ESCs) (PubMed:24623306). Associates at promoter regions of tumor suppressor genes (TSGs) leading to their gene silencing (PubMed:24623306). Promotes tumor growth (PubMed:24623306).
    Show/Hide
Uniprot ID
Primary ID:
P26358

Secondarily ID:
A0AV63
B7ZLW6
Q9UHG5
Q9ULA2
Q9UMZ6
    Show/Hide
Ensembl ID
ENSG00000130816
HGNC ID
HGNC:2976
Subcellular Location
Nucleus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000023 , BTI-Tn-5B1-4
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0429609
 Compound Info 
(2S)-2-amino-4-[[(2S,3S,4R,5R)-5-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acid
   Show/Hide
C15H21N5O5S
  1
1
IC50 = 1500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0011023
 Compound Info 
AdoHcy
   Show/Hide
C14H20N6O5S
  1
1
IC50 = 2000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0338078
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-5-(6-amino-2-fluoro-9H-purin-9-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C14H19FN6O5S
  1
1
IC50 = 2500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0302399
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-5-(6-amino-2-chloro-9H-purin-9-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C14H19ClN6O5S
  1
1
IC50 = 2900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0281849
 Compound Info 
(2-amino-4-(((2S,3S,4R,5R)-5-(6-(2-(biphenyl-4-yl)ethylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methylthio)butanoic acid)
   Show/Hide
C28H32N6O5S
  1
1
IC50 = 5400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0429610
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-5-(6-amino-2-methyl-9H-purin-9-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C15H22N6O5S
  1
1
IC50 = 6000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0455274
 Compound Info 
2-Amino-4-{(2S,3S,4R,5R)-5-[6-(2-biphenyl-4-yl-ethylamino)-2-chloro-purin-9-yl]-3,4-dihydroxy-tetrahydro-furan-2-ylmethylsulfanyl}-butyric acid
   Show/Hide
C28H31ClN6O5S
  1
1
IC50 = 6700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0498808
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-3,4-dihydroxy-5-(6-(3-phenylpropylamino)-9H-purin-9-yl)-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C23H30N6O5S
  1
1
IC50 = 7400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0429613
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-5-(7-amino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C13H19N7O5S
  1
1
IC50 = 8000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0475851
 Compound Info 
4-(((2S,3S,4R,5R)-5-(6-(3,5-dimethoxybenzylamino)-9H-purin-9-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl)methylthio)-2-aminobutanoic acid
   Show/Hide
C23H30N6O7S
  1
1
IC50 = 18000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0429614
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-5-(6-amino-2-iodo-9H-purin-9-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C14H19IN6O5S
  1
1
IC50 = 21000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0455272
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-3,4-dihydroxy-5-(6-(pyridin-4-ylmethylamino)-9H-purin-9-yl)-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C20H25N7O5S
  1
1
IC50 = 22000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0457502
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-3,4-dihydroxy-5-(6-(phenethylamino)-9H-purin-9-yl)-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C22H28N6O5S
  1
1
IC50 = 27000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0457501
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-5-(4-amino-1H-imidazo[4,5-c]pyridin-1-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C15H21N5O5S
  1
1
IC50 = 45000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0492257
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-5-(7-amino-3H-imidazo[4,5-b]pyridin-3-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C15H21N5O5S
  1
1
IC50 = 45000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0397034
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-5-(6-(benzylamino)-9H-purin-9-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C21H26N6O5S
  1
1
IC50 = 61000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0498809
 Compound Info 
2-amino-4-(((2S,3S,4R,5R)-5-(6-amino-2-methoxy-9H-purin-9-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl)methylthio)butanoic acid
   Show/Hide
C15H22N6O6S
  1
1
IC50 = 75000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0019422
 Compound Info 
N-[4-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl]-4-(quinolin-4-ylamino)benzamide
   Show/Hide
C27H23N7O
  7
1 EC50 = 10200 nM
2 IC50 = 850 nM
3 IC50 = 3550 nM
4 IC50 = 6000 nM
5 IC50 = 11220 nM
6 IC50 = 12500 nM
7 IC50 = 35000 nM
CP0011023
 Compound Info 
AdoHcy
   Show/Hide
C14H20N6O5S
  6
1 IC50 = 71 nM
2 IC50 = 200 nM
3 IC50 = 600 nM
4 IC50 = 800 nM
5 IC50 = 900 nM
6 IC50 = 941 nM
CP0029808
 Compound Info 
N-[3-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl]-3-(quinolin-4-ylamino)benzamide
   Show/Hide
C27H23N7O
  2
1 IC50 = 120 nM
2 IC50 = 9000 nM
CP0033640
 Compound Info 
6-methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-amine
   Show/Hide
C28H38N4O3
  1
1 IC50 = 382 nM
CP0281849
 Compound Info 
(2-amino-4-(((2S,3S,4R,5R)-5-(6-(2-(biphenyl-4-yl)ethylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methylthio)butanoic acid)
   Show/Hide
C28H32N6O5S
  1
1 IC50 = 5400 nM
Clinical Information about the Protein
Target 1 ( DNA [cytosine-5]-methyltransferase 1 (DNMT1) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Myelodysplastic syndrome [ICD-11: 2A37]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 CC-486
 Drug Info 
Phase 3
Myelodysplastic syndrome
Target 2 ( HUMAN DNA [cytosine-5]-methyltransferase 1 (DNMT1) )
Target Type Unknown Type Target