DNA Methyltransferase

Signaling Pathway Map

Research Area

Inhibitory Selectivity

DNA Methyltransferase Products

Catalog No. Information Product Use Citations Product Validations
S1200

Decitabine

Decitabine is a DNA methyltransferase inhibitor, incorporating into DNA and resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. It is used to treat myelodysplastic syndrome (MDS). Decitabine induces cell cycle arrest and apoptosis in various cancer cell lines.

S1782

Azacitidine (5-Azacytidine)

Azacitidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.

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.

S2477New

2'-Deoxy-5-Fluorocytidine

2'-Deoxy-5-fluorocytidine, a pyrimidine analog, is a DNA methyltransferase (DMNT) inhibitor currently in clinical trials for solid tumors.

S8812New

CM272

CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death.

S6682New

Bobcat339 hydrochloride

Bobcat339 is a selective cytosine-based TET enzyme inhibitor with IC50 of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 can reduce DNA 5-hydroxymethylcytosine abundance by inhibiting TET enzyme function in living cells and provide support for its utility as a viable pharmacological probe.

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. SGI‑1027 induces apoptosis.

S3957

Gamma-Oryzanol

Gamma-oryzanol (GO), a nutriactive phytochemical naturally occurring in crude rice bran oil, is an antioxidant compound used to treat hyperlipidemia, disorders of menopause and to increase the muscle mass. 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).

S2250

(-)-Epigallocatechin Gallate

(-)-Epigallocatechin Gallate(EGCG) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.

S4771

β-thujaplicin

β-Thujaplicin (β-TH, Hinokitiol) is a toxic tropolone derivative present in the heartwood of western red cedar (Thuja plicata) and is used as a preservative and antimicrobial additive in a number of commercial goods. Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.

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 DNA methyltransferase inhibitor, incorporating into DNA and resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. It is used to treat myelodysplastic syndrome (MDS). Decitabine induces cell cycle arrest and apoptosis in various cancer cell lines.

S1782

Azacitidine (5-Azacytidine)

Azacitidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.

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.

S2477New

2'-Deoxy-5-Fluorocytidine

2'-Deoxy-5-fluorocytidine, a pyrimidine analog, is a DNA methyltransferase (DMNT) inhibitor currently in clinical trials for solid tumors.

S8812New

CM272

CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death.

S6682New

Bobcat339 hydrochloride

Bobcat339 is a selective cytosine-based TET enzyme inhibitor with IC50 of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 can reduce DNA 5-hydroxymethylcytosine abundance by inhibiting TET enzyme function in living cells and provide support for its utility as a viable pharmacological probe.

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. SGI‑1027 induces apoptosis.

S3957

Gamma-Oryzanol

Gamma-oryzanol (GO), a nutriactive phytochemical naturally occurring in crude rice bran oil, is an antioxidant compound used to treat hyperlipidemia, disorders of menopause and to increase the muscle mass. 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).

S2250

(-)-Epigallocatechin Gallate

(-)-Epigallocatechin Gallate(EGCG) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.

S4771

β-thujaplicin

β-Thujaplicin (β-TH, Hinokitiol) is a toxic tropolone derivative present in the heartwood of western red cedar (Thuja plicata) and is used as a preservative and antimicrobial additive in a number of commercial goods. Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.

S4294

Procainamide HCl

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