DNA Methyltransferase

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No. Information Product Use Citations Product Validations
S1200

Decitabine

Decitabine is a potent inhibitor of DNA methylation, used to treat myelodysplastic syndrome (MDS).

S1782

Azacitidine

Azacitidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases.

S2821

RG108

RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, does not cause trapping of covalent enzymes.

S7113

Zebularine

Zebularine is a DNA methylation inhibitor that forms a covalent complex with DNA methyltransferases, also inhibits cytidinedeaminase with Ki of 2 μM in a cell-free assay.

S1774

Thioguanine

Thioguanine, a purine antimetabolite, inhibits DNMT1 activity through ubiquitin-targeted degradation, used in the treatment of acute lymphoblastic leukemia, autoimmune disorders (e.g., Crohn's disease, rheumatoid arthritis) and organ transplant recipients.

S7276

SGI-1027

SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B in cell-free assays, respectively.

S8056

Lomeguatrib

Lomeguatrib is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM.

S4294

Procainamide HCl

Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.

Catalog No. Information Product Use Citations Product Validations
S1200

Decitabine

Decitabine is a potent inhibitor of DNA methylation, used to treat myelodysplastic syndrome (MDS).

S1782

Azacitidine

Azacitidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases.

S2821

RG108

RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, does not cause trapping of covalent enzymes.

S7113

Zebularine

Zebularine is a DNA methylation inhibitor that forms a covalent complex with DNA methyltransferases, also inhibits cytidinedeaminase with Ki of 2 μM in a cell-free assay.

S1774

Thioguanine

Thioguanine, a purine antimetabolite, inhibits DNMT1 activity through ubiquitin-targeted degradation, used in the treatment of acute lymphoblastic leukemia, autoimmune disorders (e.g., Crohn's disease, rheumatoid arthritis) and organ transplant recipients.

S7276

SGI-1027

SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B in cell-free assays, respectively.

S8056

Lomeguatrib

Lomeguatrib is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM.

S4294

Procainamide HCl

Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.