DNA methylation, defined by the addition of a methyl group to adenine or cytosine bases in DNA catalyzed by DNA methyltransferases (MTases), is one of the most studied post-replicative DNA modification mechanism in bacteria. The three forms of nucleotide methylation identified to date are: N6-methyladenine(m6A), N4-methylcytosine (m4C), and 5-methylcytosine (m5C). DNA methylation, one type of epigenetic modification, represses gene expression. DNA methylation is caused primarily by a family of DNA methyltransferases (DNMTs) including DNMT1, DNMT3a and DNMT3b. Conventionally, DNMT1 acts as the primary maintenance methyltransferase to keep the methylation of DNA that is already established at the genome, whereas DNMT3a and DNMT3b are classified asde novo methyltransferases to reversibly methylate unmethylated DNA. DNA methylation represses gene transcription through several mechanisms including physically blocking the binding of transcription factors and/or functioning as docking sites for transcriptional repressors/corepressors. In epigenetic transcriptional regulation, which is important for embryonic development, DNA-methylation patterns are determined by de novo methylation by the DNA methyltransferases Dnmt3a and Dnmt3b in the embryo. DNA methylation on the cytosine of CpGdinucleotides in gene promoter regions is associated with silencing gene expression. Of the DNA methyltransferases, only DNA methyltransferase 3a (DNMT3a) and 3b (DNMT3b) are capable of adding de novo CpG methylation marks and thus may dynamically regulate gene silencing.


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Zebularine

Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor; also an inhibitor of cytidine deaminase with a Ki of 0.95 μM.

  • CAS Number: 3690-10-6
  • MF: C9H12N2O5
  • MW: 228.202
  • Catalog: Autophagy
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: 499.0±55.0 °C at 760 mmHg
  • Melting Point: 160-162?C
  • Flash Point: 255.6±31.5 °C

GSK3735967

GSK3735967 is a potent, selective, non-nucleoside inhibitor of DNMT1 with IC50 of 40 nM.

  • CAS Number: 2170136-86-2
  • MF: C25H31N7Os
  • MW: 477.631
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Psammaplin A

Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity[1][2].

  • CAS Number: 110659-91-1
  • MF: C22H24Br2N4O6S2
  • MW: 664.38700
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ZIKV-IN-2

ZIKV-IN-2 (compound 3a) is a potent ZIKV NS5 methyl transferase (MTase) inhibitor with an IC50 value of 38.86 μM. ZIKV-IN-2 inhibits ZIKV replication and infection. ZIKV-IN-2 can be used in research of Zika virus (ZIKV)[1].

  • CAS Number: 910582-16-0
  • MF: C39H42O4
  • MW: 574.75
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2′-Deoxy-5-nitrocytidine

2′-Deoxy-5-nitrocytidine is a DNA Methyltransferase inhibitor extracted from patent CN108498529A. 2′-Deoxy-5-nitrocytidine can be used for the research of cancer[1].

  • CAS Number: 69100-02-3
  • MF: C9H12N4O6
  • MW: 272.21
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

procainamide

Procainamide is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1). Procainamide is a Class 1A antiarrhythmic agent. Procainamide has the potential for the research of cancer and arrhythmias[1][2].

  • CAS Number: 51-06-9
  • MF: C13H21N3O
  • MW: 235.32500
  • Catalog: Bacterial
  • Density: 1.06
  • Boiling Point: 421.8ºC at 760mmHg
  • Melting Point: 47°C
  • Flash Point: 208.9ºC

DY-46-2

DY-46-2 is a high potency and selectivity novel non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor with an IC50 value of 0.39 μM[1].

  • CAS Number: 1105110-83-5
  • MF: C19H22N6O5S
  • MW: 446.48
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SGI 1027

SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.

  • CAS Number: 1020149-73-8
  • MF: C27H23N7O
  • MW: 461.518
  • Catalog: DNA Methyltransferase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: >280℃
  • Flash Point: N/A

Bobcat 339

Bobcat339 (Bobcat 339) is a novel cytosine-based TET enzyme inhibitor with IC50 of 33 uM (TET1) and 73 uM (TET2), but not DNMT3a, does not inhibit the DNA methyltransferase DNMT3a; Bobcat339 is a useful tool for investigation of epigenetics and serve as a starting point for new therapeutics that target DNA methylation and gene transcription.

  • CAS Number: 2280037-51-4
  • MF: C16H12ClN3O
  • MW: 297.742
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HaeIII Methyltransferase

HaeIII Methyltransferase (HaeIII) is a Methyltransferase which can bind covalently to DNA[1].

  • CAS Number: 92228-40-5
  • MF:
  • MW:
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2',3',5'-triacetyl-5-Azacytidine

2′,3′,5′-Triacetyl-5-azacytidine is an orally active prodrug of 5-Azacytidine. 5-Azacytidine is an inhibitor of DNA methyltransferase[1].

  • CAS Number: 10302-78-0
  • MF: C14H18N4O8
  • MW: 370.315
  • Catalog: DNA Methyltransferase
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 497.3±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 254.6±31.5 °C

5-Aza-4'-thio-2'-deoxycytidine

5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects[1].

  • CAS Number: 169514-76-5
  • MF: C8H12N4O3S
  • MW: 244.27
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CM-579

CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells[1].

  • CAS Number: 1846570-40-8
  • MF: C29H40N4O3
  • MW: 492.65
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dihydro-5-azacytidine

Dihydro-5-azacytidine (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine has an antitumor activity[1][2].

  • CAS Number: 62488-57-7
  • MF: C8H14N4O5
  • MW: 246.221
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.1±0.1 g/cm3
  • Boiling Point: 529.1ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 273.8ºC

DNMT3A-IN-1

DNMT3A-IN-1 is a potent and selective DNMT3A inhibitor. DNMT3A-IN-1 shows inhibitor activities against DNMT3A with kI values range from 9.16-18.85 μM (AdoMet) and 11.37-23.34 μM (poly dI-dC) [1].

  • CAS Number: 1403598-56-0
  • MF: C30H38N6O4
  • MW: 546.66
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SGI-110

Guadecitabine (SGI-110) is a DNA methyltransferases (DNMT) inhibitor.

  • CAS Number: 929901-49-5
  • MF: C18H24N9O10P
  • MW: 557.411
  • Catalog: DNA Methyltransferase
  • Density: 2.2±0.1 g/cm3
  • Boiling Point: 956.4±75.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 532.2±37.1 °C

RG108

RG108 is a non-nucleoside inhibitor of DNA methyltransferase with an IC50 of 115 nM.

  • CAS Number: 48208-26-0
  • MF: C19H14N2O4
  • MW: 334.326
  • Catalog: DNA Methyltransferase
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 606.0±50.0 °C at 760 mmHg
  • Melting Point: 192-194℃
  • Flash Point: 320.3±30.1 °C

γ-Oryzanol

γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of DNMT1 (IC50=3.2 μM), DNMT3a (IC50=22.3 μM).

  • CAS Number: 11042-64-1
  • MF: C40H58O4
  • MW: 602.886
  • Catalog: DNA Methyltransferase
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 663.2±40.0 °C at 760 mmHg
  • Melting Point: 135-137°C
  • Flash Point: 193.8±20.8 °C

ZIKV-IN-3

ZIKV-IN-3 (compound 5a), an andrographolide derivatives, is a potent ZIKV NS5 methyl transferase (MTase) inhibitor with an IC50 value of 18.34 μM. ZIKV-IN-3 inhibits ZIKV replication and infection. ZIKV-IN-3 can be used in research of Zika virus (ZIKV)[1].

  • CAS Number: 947699-46-9
  • MF: C39H41NO4
  • MW: 587.75
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CpG Methyltransferase

CpG Methyltransferase is a DNA methyltransferase. CpG Methyltransferase can methylate the C5 position on the base moiety of all cytosine nucleotides contained in unmethylated or hemimethylated double stranded DNA in a 5’-CpG-3’ context[1].

  • CAS Number: 1809633-78-0
  • MF:
  • MW:
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hhal Methyltransferase

Hhal Methyltransferase (Hhal) is a DNA methyltransferase (recognition sequence: GCGC)[1].

  • CAS Number: 91448-96-3
  • MF:
  • MW:
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dihydro-5-azacytidine acetate

Dihydro-5-azacytidine acetate (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine acetate has an antitumor activity[1][2].

  • CAS Number: 2470972-18-8
  • MF: C10H18N4O7
  • MW: 306.27
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DNMT-IN-3

DNMT-IN-3 is an DNA Methyltransferase (DNMT) inhibitor, and plays an antimalarial role with IC50 of 60 nM against Plasmodium falciparum (Plasmodium). DNMT-IN-3 can be used for malaria related research[1].

  • CAS Number: 1683516-27-9
  • MF: C37H39N7O
  • MW: 597.75
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

6-Methyl-5-azacytidine

6-Methyl-5-azacytidine is a potent DNMT inhibitor.

  • CAS Number: 105330-94-7
  • MF: C9H14N4O5
  • MW: 258.23
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GSK-3484862

GSK-3484862 is a non-covalent inhibitor for Dnmt1. GSK-3484862 induces DNA hypomethylation to against cancer[1].

  • CAS Number: 2170136-65-7
  • MF: C19H19N5OS
  • MW: 365.45
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

EcoRI Methyltransferase

EcoRI Methyltransferase is a bacterial sequence-specific S-adenosyl-L-methionine-dependent DNA methyltransferase. EcoRI Methyltransferase relies on a complex conformational mechanism to achieve its remarkable specificity, including DNA bending, base flipping and intercalation into the DNA[1].

  • CAS Number: 81458-00-6
  • MF:
  • MW:
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DC-05

DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 10.3 μM and 1.09 μM, respectively.

  • CAS Number: 890643-16-0
  • MF: C25H25N3O
  • MW: 383.486
  • Catalog: DNA Methyltransferase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 667.5±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 357.5±31.5 °C

SW155246

SW155246 is a DNA methyltransferase (DNMT1) selective inhibitor with IC50s of 1.2 and 38 μM for hDNMT1 and mDNMT3A, respectively. SW155246 can be used for the research of cancer and other diseases[1].

  • CAS Number: 420092-79-1
  • MF: C16H11ClN2O5S
  • MW: 378.787
  • Catalog: DNA Methyltransferase
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 613.2±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 324.6±34.3 °C

DC_517

DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively.

  • CAS Number: 500017-70-9
  • MF: C33H35N3O2
  • MW: 505.650
  • Catalog: DNA Methyltransferase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 727.9±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 394.0±32.9 °C

SGI-110

S-110 is a dinucleotide consisting of 5-Aza-CdR followed by a deoxyguanosine which shows to be an effective DNA methylation inhibitor.

  • CAS Number: 929904-85-8
  • MF: C18H23N9NaO10P
  • MW: 579.39300
  • Catalog: DNA Methyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A