Page last updated: 2024-11-13

sgi-1027

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Description

SGI-1027: inhibits DNA methyltransferase 1; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID24858111
CHEMBL ID2336409
SCHEMBL ID3655385
MeSH IDM0584948

Synonyms (40)

Synonym
bdbm50430056
S7276
CHEMBL2336409 ,
1020149-73-8
sgi-1027
FD5030
HY-13962
SCHEMBL3655385
n-[4-[(2-amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide
sgi 1027
AC-33115
AKOS024458519
n-[4-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl]-4-(quinolin-4-ylamino)benzamide
gtpl8891
J-000537
mfcd27937047
dna methyltransferase inhibitor ii
sgi1027
n-(4-((2-amino-6-methylpyrimidin-4-yl)amino)phenyl)-4-(quinolin-4-ylamino)benzamide
HMS3653O06
n-{4-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl}-4-[(quinolin-4-yl)amino]benzamide
AS-74078
sgi-1027, >=98% (hplc)
NCGC00381561-65
SW220204-1
benzamide, n-[4-[(2-amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)-
FT-0755513
EX-A2160
Q27088794
1020086-21-8
BCP09928
SB19043
HMS3748A21
CCG-269354
A857823
nsc-783333
nsc783333
VQB14973
EN300-189631
Z1880962221

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency8.48660.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency13.45040.00108.379861.1304AID1645840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Myc proto-oncogene proteinHomo sapiens (human)IC50 (µMol)7.31001.00005.73259.6700AID1777418; AID1777419; AID1777435
CPG DNA methylaseSpiroplasma monobiaeIC50 (µMol)1.60000.00280.55821.6000AID1802375
DNA (cytosine-5)-methyltransferase 1Homo sapiens (human)IC50 (µMol)9.59000.01861.64886.0000AID1073770; AID1073771; AID1199269; AID1505769; AID1505821; AID1505822; AID1802375; AID736572
Dual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)IC50 (µMol)7.31000.00254.38999.6700AID1777418; AID1777419; AID1777435
Histone-lysine N-methyltransferase EHMT2Homo sapiens (human)IC50 (µMol)34.50000.00251.14809.2000AID1505768; AID1505823
Histone-lysine N-methyltransferase EHMT1Homo sapiens (human)IC50 (µMol)65.00000.01300.79954.9000AID1073764
DNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)IC50 (µMol)7.50000.20001.21647.5000AID1199271
DNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)IC50 (µMol)10.00000.50003.966710.0000AID1073769
DNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)IC50 (µMol)5.12500.50003.733310.0000AID1073769; AID1199270; AID1664320; AID1802375
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)EC50 (µMol)0.90000.90000.90000.9000AID1240593
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (114)

Processvia Protein(s)Taxonomy
positive regulation of cell population proliferationMyc proto-oncogene proteinHomo sapiens (human)
regulation of gene expressionMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationMyc proto-oncogene proteinHomo sapiens (human)
G1/S transition of mitotic cell cycleMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIMyc proto-oncogene proteinHomo sapiens (human)
MAPK cascadeMyc proto-oncogene proteinHomo sapiens (human)
branching involved in ureteric bud morphogenesisMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of mesenchymal cell proliferationMyc proto-oncogene proteinHomo sapiens (human)
chromatin remodelingMyc proto-oncogene proteinHomo sapiens (human)
intracellular iron ion homeostasisMyc proto-oncogene proteinHomo sapiens (human)
DNA damage responseMyc proto-oncogene proteinHomo sapiens (human)
response to xenobiotic stimulusMyc proto-oncogene proteinHomo sapiens (human)
response to gamma radiationMyc proto-oncogene proteinHomo sapiens (human)
regulation of cell cycle processMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of gene expressionMyc proto-oncogene proteinHomo sapiens (human)
regulation of telomere maintenanceMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of stress-activated MAPK cascadeMyc proto-oncogene proteinHomo sapiens (human)
protein-DNA complex disassemblyMyc proto-oncogene proteinHomo sapiens (human)
cellular response to UVMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of apoptotic processMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processMyc proto-oncogene proteinHomo sapiens (human)
fibroblast apoptotic processMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of monocyte differentiationMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of DNA-templated transcriptionMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of fibroblast proliferationMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of fibroblast proliferationMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of epithelial cell proliferationMyc proto-oncogene proteinHomo sapiens (human)
chromosome organizationMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of cell divisionMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of telomerase activityMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of transcription initiation by RNA polymerase IIMyc proto-oncogene proteinHomo sapiens (human)
ERK1 and ERK2 cascadeMyc proto-oncogene proteinHomo sapiens (human)
response to growth factorMyc proto-oncogene proteinHomo sapiens (human)
cellular response to hypoxiaMyc proto-oncogene proteinHomo sapiens (human)
cellular response to xenobiotic stimulusMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of metanephric cap mesenchymal cell proliferationMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathway by p53 class mediatorMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of miRNA transcriptionMyc proto-oncogene proteinHomo sapiens (human)
regulation of somatic stem cell population maintenanceMyc proto-oncogene proteinHomo sapiens (human)
regulation of transcription by RNA polymerase IIMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of cell population proliferationMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
DNA-templated transcriptionDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
positive regulation of gene expressionDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
negative regulation of gene expressionDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
methylationDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
epigenetic programming of gene expressionDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
cellular response to amino acid stimulusDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
chromosomal DNA methylation maintenance following DNA replicationDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
cellular response to bisphenol ADNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
negative regulation of vascular associated smooth muscle cell apoptotic processDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
negative regulation of vascular associated smooth muscle cell differentiation involved in phenotypic switchingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
regulation of cytokine productionDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
response to ischemiaDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
inflammatory responseDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
signal transductionDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
heart developmentDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
stress-activated protein kinase signaling cascadeDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
negative regulation of hippo signalingDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
p38MAPK cascadeDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
positive regulation of MAPK cascadeDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
positive regulation of protein kinase activityDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
positive regulation of DNA-templated transcriptionDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
cardiac muscle contractionDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
cellular response to lipopolysaccharideDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
cellular response to sorbitolDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
cellular senescenceDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
MAPK cascadeDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
cellular response to starvationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
regulation of DNA replicationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
synaptonemal complex assemblyHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
spermatid developmentHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
long-term memoryHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
fertilizationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
peptidyl-lysine dimethylationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
regulation of protein modification processHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
organ growthHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
phenotypic switchingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
response to ethanolHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
behavioral response to cocaineHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
oocyte developmentHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
neuron fate specificationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
response to fungicideHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
cellular response to cocaineHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
cellular response to xenobiotic stimulusHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
negative regulation of autophagosome assemblyHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
chromatin organizationHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
peptidyl-lysine monomethylationHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
peptidyl-lysine dimethylationHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
regulation of embryonic developmentHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
response to fungicideHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
positive regulation of cold-induced thermogenesisHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
positive regulation of gene expressionDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
methylationDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
placenta developmentDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
DNA methylation-dependent heterochromatin formationDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
male meiosis IDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
spermatogenesisDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
methylationDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
epigenetic programing of female pronucleusDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
negative regulation of gene expression, epigeneticDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
stem cell differentiationDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
chorionic trophoblast cell differentiationDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
genomic imprintingDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
negative regulation of DNA methylation-dependent heterochromatin formationDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
retrotransposon silencing by heterochromatin formationDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
autosome genomic imprintingDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
DNA methylation-dependent heterochromatin formationDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
spermatogenesisDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
response to xenobiotic stimulusDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
response to toxic substanceDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
response to ionizing radiationDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
response to lead ionDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
neuron differentiationDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
regulatory ncRNA-mediated heterochromatin formationDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
methylationDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
response to estradiolDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
response to vitamin ADNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
response to cocaineDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
S-adenosylmethionine metabolic processDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
cellular response to amino acid stimulusDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
cellular response to ethanolDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
cellular response to hypoxiaDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
hepatocyte apoptotic processDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
autosome genomic imprintingDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
positive regulation of cellular response to hypoxiaDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
cellular response to bisphenol ADNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
negative regulation of DNA-templated transcriptionDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (46)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingMyc proto-oncogene proteinHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificMyc proto-oncogene proteinHomo sapiens (human)
core promoter sequence-specific DNA bindingMyc proto-oncogene proteinHomo sapiens (human)
transcription coregulator bindingMyc proto-oncogene proteinHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificMyc proto-oncogene proteinHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificMyc proto-oncogene proteinHomo sapiens (human)
DNA bindingMyc proto-oncogene proteinHomo sapiens (human)
protein bindingMyc proto-oncogene proteinHomo sapiens (human)
identical protein bindingMyc proto-oncogene proteinHomo sapiens (human)
protein-containing complex bindingMyc proto-oncogene proteinHomo sapiens (human)
protein dimerization activityMyc proto-oncogene proteinHomo sapiens (human)
E-box bindingMyc proto-oncogene proteinHomo sapiens (human)
DNA-binding transcription factor bindingMyc proto-oncogene proteinHomo sapiens (human)
SCF ubiquitin ligase complex bindingMyc proto-oncogene proteinHomo sapiens (human)
DNA bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
RNA bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
DNA (cytosine-5-)-methyltransferase activityDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
protein bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
zinc ion bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
methyl-CpG bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
DNA-methyltransferase activityDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
promoter-specific chromatin bindingDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
protein serine/threonine kinase activityDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
MAP kinase kinase activityDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
protein tyrosine kinase activityDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
protein bindingDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
ATP bindingDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
protein kinase bindingDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
protein serine kinase activityDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
transcription corepressor bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
p53 bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
protein bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
zinc ion bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
protein-lysine N-methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
enzyme bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K9 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K27 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
C2H2 zinc finger domain bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K56 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K9me2 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
promoter-specific chromatin bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
transcription corepressor bindingHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
p53 bindingHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
protein bindingHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
methyltransferase activityHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
zinc ion bindingHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
protein-lysine N-methyltransferase activityHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
histone H3K9 methyltransferase activityHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
histone H3K27 methyltransferase activityHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
C2H2 zinc finger domain bindingHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
histone H3K9me2 methyltransferase activityHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
transcription corepressor activityDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
DNA (cytosine-5-)-methyltransferase activityDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
protein bindingDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
DNA-methyltransferase activityDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
metal ion bindingDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
DNA (cytosine-5-)-methyltransferase activity, acting on CpG substratesDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
DNA bindingDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
protein bindingDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
enzyme activator activityDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
enzyme bindingDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
metal ion bindingDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
DNA (cytosine-5-)-methyltransferase activity, acting on CpG substratesDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
DNA bindingDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
DNA bindingDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
chromatin bindingDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
transcription corepressor activityDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
DNA (cytosine-5-)-methyltransferase activityDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
protein bindingDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
identical protein bindingDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
unmethylated CpG bindingDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
metal ion bindingDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
lncRNA bindingDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
protein-cysteine methyltransferase activityDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
nucleusMyc proto-oncogene proteinHomo sapiens (human)
nucleoplasmMyc proto-oncogene proteinHomo sapiens (human)
nucleolusMyc proto-oncogene proteinHomo sapiens (human)
cytoplasmMyc proto-oncogene proteinHomo sapiens (human)
Myc-Max complexMyc proto-oncogene proteinHomo sapiens (human)
RNA polymerase II transcription repressor complexMyc proto-oncogene proteinHomo sapiens (human)
chromatinMyc proto-oncogene proteinHomo sapiens (human)
protein-containing complexMyc proto-oncogene proteinHomo sapiens (human)
female germ cell nucleusDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
nucleusDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
nucleoplasmDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
replication forkDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
pericentric heterochromatinDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
nucleusDNA (cytosine-5)-methyltransferase 1Homo sapiens (human)
cytoplasmDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
nucleoplasmDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
cytosolDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
membraneDual specificity mitogen-activated protein kinase kinase 3Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
nucleoplasmHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
nuclear speckHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
chromatinHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
nucleoplasmHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
nuclear bodyHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
chromatinHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
nucleusDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
nucleoplasmDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
catalytic complexDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
nucleusDNA (cytosine-5)-methyltransferase 3BHomo sapiens (human)
ESC/E(Z) complexDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
condensed nuclear chromosomeDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
nucleusDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
cytosolDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
catalytic complexDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
heterochromatinDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
nucleusDNA (cytosine-5)-methyltransferase 3-likeHomo sapiens (human)
chromosome, centromeric regionDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
XY bodyDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
nucleusDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
nucleoplasmDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
cytoplasmDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
nuclear matrixDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
catalytic complexDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
euchromatinDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
heterochromatinDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
nucleusDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
cytoplasmDNA (cytosine-5)-methyltransferase 3AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (75)

Assay IDTitleYearJournalArticle
AID1777425Disruption of MKK3/MYC protein-protein interaction in human HCT-116 cells transfected with VF-tagged MKK3 assessed as inhibition of MYC transcriptional activity at 0.5 to 2 uM measured after 12 hrs by Renilla luciferase based reporter assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1654637Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs in presence of AOX inhibitor hydralazine by UPLC/Q-TOF MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID1240602Antiproliferative activity against human KARPAS299 cells after 2 to 4 days by ATPlite 1step luminescence assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design and synthesis of new non nucleoside inhibitors of DNMT3A.
AID736571Cell cycle arrest in human U937 cells at 5 to 50 uM after 30 hrs by FACS analysis2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.
AID1777428Inhibition of cell migration in human HCT-116 cells measured after 18 hrs by scratch wound healing assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1169763Binding affinity to DNA (unknown origin) at 0.0625 to 0.5 mM by ethidium bromide dye based agarose gel electrophoresis method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening.
AID1073758Cytotoxicity against human PC3 cells after 48 hrs by trypan blue exclusion assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1777420Disruption of interaction between human recombinant GST-tagged MKK3/VF-tagged p38 expressed in HEK293T cells at 50 uM incubated for 30 mins by GST pull-down assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1777424Disruption of MKK3/MYC protein-protein interaction in human MDA-MB-468 cells assessed as decrease in MYC level at 1 to 20 uM measured by western blot assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1073766Inhibition of rat recombinant PRMT1 using histone as substrate preincubated for 5 mins followed by substrate addition measured after 6.5 mins by liquid scintillation counting analysis in presence of [methyl-3H]-AdoMet2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1654632Substrate activity at aldehyde oxidase in human liver cytosol at 10 uM measured after 3 hrs by UPLC/Q-TOF MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID1777422Disruption of MKK3/MYC protein-protein interaction in human HCT-116 cells assessed as decrease in CDK4 level at 0.5 to 10 uM measured by western blot assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1073770Inhibition of human N-terminal 600 residues-deleted DNMT1 using hemimethylated (GAC)12 as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins by liquid scintillation counting analysis in presence of [methyl-3H]-AdoMet2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1777434Disruption of interaction between human recombinant GST-tagged MKK3 expressed in HEK293T cells/MYC in human HCT116 cells incubated for 30 mins by GST pull-down assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1777437Disruption of MKK3/MYC protein-protein interaction in human MDA-MB-468 cells assessed as decrease in CDK4 level at 1 to 20 uM measured by western blot assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1777429Inhibition of cell migration in human HCT-116 cells assessed as relative wound density at 3 uM measured after 18 hrs by scratch wound healing assay (Rvb = 20%)2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID750165Cytotoxicity against human HCT116 cells assessed as viability2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Structure-activity relationships for 4-anilinoquinoline derivatives as inhibitors of the DNA methyltransferase enzyme DNMT1.
AID1447858Inhibition of human DNMT3A catalytic domain using AdoMet assessed as reduction of methylation in 5'-biotin/3' 6-carboxyfluorescein labeled DNA duplex at CpG site at 32 uM after 1 hr by fluorescence assay relative to control2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Rational Design of Bisubstrate-Type Analogues as Inhibitors of DNA Methyltransferases in Cancer Cells.
AID1073765Selectivity ratio of IC50 for rat recombinant PRMT1 to IC50 for human N-terminal 600 residues-deleted DNMT12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1452276Antiproliferative activity against human U937 cells after 72 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors.
AID750164Inhibition of DNMT1 in human HCT116 cells at 5 uM after 24 hrs by Western blot analysis relative to control2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Structure-activity relationships for 4-anilinoquinoline derivatives as inhibitors of the DNA methyltransferase enzyme DNMT1.
AID1199271Inhibition of His6-tagged human recombinant DNMT3b expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scinti2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Targeting DNA methylation with small molecules: what's next?
AID1777426Disruption of MKK3/MYC protein-protein interaction in human MDA-MB-468 cells transfected with VF-tagged MKK3 assessed as inhibition of MYC transcriptional activity measured after 12 hrs by Renilla luciferase based reporter assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1777419Disruption of interaction between human recombinant GST-tagged MKK3 (1 to 210 residues)/VF-tagged MYC expressed in HEK293T cells measured after 2 hrs by TR-FRET assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1199269Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Targeting DNA methylation with small molecules: what's next?
AID1777421Disruption of MKK3/MYC protein-protein interaction in human HCT-116 cells assessed as decrease in MYC level at 0.5 to 10 uM measured by western blot assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1505768Inhibition of human G9a using biotinylated-H3K9 peptide as substrate after 1 hr in presence of SAM by TR-FRET assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.
AID1777439Inhibition of Renilla luciferase activity expressed in human HCT-116 cells assessed as decrease in luminescence at 10 uM measured after 12 hrs by luminescence assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1073763Selectivity ratio of IC50 for human GLP (734 to 1235) to IC50 for human N-terminal 600 residues-deleted DNMT12014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1777418Disruption of interaction between human recombinant GST-tagged MKK3/VF-tagged MYC expressed in HEK293T cells measured after 2 hrs by TR-FRET assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1654634Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs by LC-MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID736573Inhibition of human DNMT1 using AdoMet and poly dI-dC at 50 uM after 2 hrs by radioactive assay2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.
AID1240596Inhibition of human His-DNMT1 using [methyl-3H]SAM as substrate after 2 hrs2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design and synthesis of new non nucleoside inhibitors of DNMT3A.
AID1654638Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs in presence of XO inhibitor allopurinol by UPLC/Q-TOF MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID1777430Disruption of interaction between human recombinant GST-tagged MKK3/VF-tagged MYC expressed in HEK293T cells at 20 uM measured after 2 hrs by TR-FRET assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID736572Inhibition of human DNMT1 using AdoMet and poly dI-dC after 2 hrs by radioactive assay2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.
AID1777436Inhibition of MKK3 in human HEK293T cells assessed as inhibition of p38 phosphorylation by western blot analysis2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1447861Inhibition of full length His-tagged human DNMT1 using SAM/[methyl-3H]SAM assessed as reduction of methylation in biotinylated hemimethylated DNA duplex at 100 uM after 1 hr by scintillation counting method relative to control2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Rational Design of Bisubstrate-Type Analogues as Inhibitors of DNA Methyltransferases in Cancer Cells.
AID1654636Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs in presence of AOX inhibitor raloxifene by UPLC/Q-TOF MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID1505769Inhibition of human DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate after 15 mins in presence of SAM by TR-FRET assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.
AID1073771Inhibition of human N-terminal 600 residues-deleted DNMT1 using poly(dI-dC) as substrate in presence of AdoMet2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1505822Inhibition of human DNMT1 using hemimethylated DNA as substrate by radioactive methyl transfer assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.
AID1777441Inhibition of Renilla luciferase activity expressed in human MDA-MB-468 cells assessed as decrease in luminescence at 10 uM measured after 12 hrs by luminescence assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1505823Inhibition of G9a (unknown origin)2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.
AID1240603Antiproliferative activity against human HCT116 cells after 2 to 4 days by ATPlite 1step luminescence assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design and synthesis of new non nucleoside inhibitors of DNMT3A.
AID1447859Inhibition of human DNMT3A catalytic domain using AdoMet assessed as reduction of methylation in 5'-biotin/3' 6-carboxyfluorescein labeled DNA duplex at CpG site at 10 uM after 1 hr by fluorescence assay relative to control2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Rational Design of Bisubstrate-Type Analogues as Inhibitors of DNA Methyltransferases in Cancer Cells.
AID1073769Inhibition of human DNMT3A2/3L using unmethylated DNA as substrate in presence of [methyl-3H]-AdoMet2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1073757Cytotoxicity against human MDA-MB-231 cells after 48 hrs by trypan blue exclusion assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1777427Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID736574Induction of apoptosis in human U937 cells assessed as accumulation at pre-G1 phase after 30 hrs by FACS analysis2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.
AID1240601Antiproliferative activity against human KG1 cells after 2 to 4 days by ATPlite 1step luminescence assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design and synthesis of new non nucleoside inhibitors of DNMT3A.
AID1777440Inhibition of cell migration in human HCT-116 cells at 0.75 to 3 uM by scratch wound healing assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1777423Disruption of MKK3/MYC protein-protein interaction in human HCT-116 cells assessed as decrease in PDL1 level at 0.5 to 10 uM measured by western blot assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1073759Cytotoxicity against human Raji cells after 48 hrs by trypan blue exclusion assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1777433Disruption of interaction between human recombinant GST-tagged MAX/VF-tagged MYC expressed in HEK293T cells at 50 uM incubated for 30 mins by GST pull-down assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1073764Inhibition of human GLP (734 to 1235) using histone as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by liquid scintillation counting analysis in presence of [methyl-3H]-AdoMet2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1777432Disruption of interaction between human recombinant GST-tagged MKK3/VF-tagged MYC expressed in HEK293T cells at 50 uM incubated for 30 mins by GST pull-down assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1452275Antiproliferative activity against human K562 cells after 72 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors.
AID1777438Disruption of MKK3/MYC protein-protein interaction in human MDA-MB-468 cells assessed as decrease in PDL1 level at 1 to 20 uM measured by western blot assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1447860Inhibition of full length His-tagged human DNMT1 using SAM/[methyl-3H]SAM assessed as reduction of methylation in biotinylated hemimethylated DNA duplex at 32 uM after 1 hr by scintillation counting method relative to control2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Rational Design of Bisubstrate-Type Analogues as Inhibitors of DNA Methyltransferases in Cancer Cells.
AID1664320Inhibition of human C-terminal DNMT3A (623 to 908 residues) using 5'-biotin labeled oligonucleotide as substrate measured after 1 hr2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1073761Cytotoxicity against human U937 cells after 48 hrs by trypan blue exclusion assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1777435Disruption of interaction between human recombinant GST-tagged MKK3/His-tagged MYC HLH LZ domain measured after 2 hrs by TR-FRET assay2021Bioorganic & medicinal chemistry, 09-01, Volume: 45Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.
AID1199270Inhibition of His6-tagged human recombinant DNMT3a expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scinti2015Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6
Targeting DNA methylation with small molecules: what's next?
AID1654635Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs by UPLC/Q-TOF MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID1505821Inhibition of human DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate by radioactive methyl transfer assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.
AID1073760Cytotoxicity against human PBMC after 48 hrs by trypan blue exclusion assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1240593Inhibition of human C-terminal DNMT3A after 1 hr by fluorescence assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design and synthesis of new non nucleoside inhibitors of DNMT3A.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346116Human DNA methyltransferase 1 (2.1.1.- Methyltransferases)2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
AID1802375DNA Methylation Assay from Article 10.1074/jbc.M113.480517: \\Laccaic acid A is a direct, DNA-competitive inhibitor of DNA methyltransferase 1.\\2013The Journal of biological chemistry, Aug-16, Volume: 288, Issue:33
Laccaic acid A is a direct, DNA-competitive inhibitor of DNA methyltransferase 1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (24)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's19 (79.17)24.3611
2020's5 (20.83)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.91

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index22.91 (24.57)
Research Supply Index3.26 (2.92)
Research Growth Index4.52 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.91)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other24 (96.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]