Dihydro-5-azacytidine (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine has an antitumor activity[1][2].
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].
Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor; also an inhibitor of cytidine deaminase with a Ki of 0.95 μM.
GSK3735967 is a potent, selective, non-nucleoside inhibitor of DNMT1 with IC50 of 40 nM.
DNMT-IN-1 is a potent DNMT inhibitor with an EC50 value of 3.2 µM. DNMT-IN-1 shows antiproliferative active[1].
Guadecitabine (SGI-110) is a DNA methyltransferases (DNMT) inhibitor.
RG108 is a non-nucleoside inhibitor of DNA methyltransferase with an IC50 of 115 nM.
6-Methyl-5-azacytidine is a potent DNMT inhibitor.
BamHI Methyltransferase is a DNA methyltransferase which modifies the underlined cytosine (GGATCC)[1].
GSK-3484862 is a non-covalent inhibitor for Dnmt1. GSK-3484862 induces DNA hypomethylation to against cancer[1].
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].
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].
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).
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].
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].
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].
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].
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].
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].
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.
DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 10.3 μM and 1.09 μM, respectively.
Benzyl selenocyanate is a chemopreventive agent for various chemically induced tumors in animal models at both the initiation and postinitiation stages. Benzyl selenocyanate is an inhibitor of DNA (cytosine-5)-methyltransferase (Mtase), with an with an IC50 of 8.4 µM[1].
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].
DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively.
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.
HaeIII Methyltransferase (HaeIII) is a Methyltransferase which can bind covalently to DNA[1].
2′,3′,5′-Triacetyl-5-azacytidine is an orally active prodrug of 5-Azacytidine. 5-Azacytidine is an inhibitor of DNA methyltransferase[1].
Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells[1]. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM[2].
S-110 is a dinucleotide consisting of 5-Aza-CdR followed by a deoxyguanosine which shows to be an effective DNA methylation inhibitor.
Hhal Methyltransferase (Hhal) is a DNA methyltransferase (recognition sequence: GCGC)[1].