SGI-1027 is a potent and selective inhibitor of DNA methyltransferase (DNMT) with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B, respectively.

DC_05 is a non-nucleoside DNMT1 inhibitor (IC50=10.3 μM) with low micromolar IC50 values and significant selectivity toward other AdoMet-dependent protein methyltransferases.

Lomeguatrib, an inhibitor of DNA repair protein O(6)-methylguanine-DNA methyltransferase (MGMT) with IC50 of 0.009 μM in cell-free extracts from HeLa S3 cells, is a modified guanine base.

5−Fluoro−2'−deoxycytidine is a DNMT inhibitor which forms covalent links with the cysteine residue in the DNMT active site.

Procainamide HCl is a blocker of sodium channel and an inhibitor of DNA methyltransferase. It is an anti-arrhythmic agent.

SU11274 is a selective Met inhibitor with IC50 of 10 nM, no effects on PGDFRβ, EGFR or Tie2.

RG108 is a DNA methyltransferase inhibitor with IC50 of 115 nM.

CM-272 is a potent, selective and reversible dual small molecule against G9a and DNMTs activity.

γ-Oryzanol is a phytochemical with membrane antioxidant, naturally occurring in crude rice bran oil, can be used to treat hyperlipidemia, disorders of menopause and to increase the muscle mass.

Zebularine is a DNA methylation inhibitor which forms a covalent complex with DNA methyltransferases, it also inhibits cytidinedeaminase with Ki of 2 μM.

Decitabine is a potent inhibitor of DNA methyltransferase with IC50 of 438 nM and 4.38 nM in HL-60 and KG1a cells, respectively.

6-Thioguanine belongs to the thiopurine family of drugs that also include mercaptopurine and azathioprine, which are examples of antimetabolites, and is a purine analogue of the nucleobase guanine. It was found to inhibit SARS-CoV PLpro. 6-Thioguanine disrupts cytosine methylation by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo.

(-)-Epigallocatechin Gallate, an antioxidant, inhibits telomerase and DNA methyltransferase. It is a polyphenol flavonoid extracted from green tea.

5-Azacytidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases.