DNA Methyltransferase

Isoform-selective Products

Signaling Pathway

DNA Methyltransferase Signaling Pathway

DNA Methyltransferase Products

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  • DNA Methyltransferase Inhibitors (15)
  • New DNA Methyltransferase Products
Catalog No. Product Name 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.
Cell Rep Med, 2024, 5(2):101416
NPJ Precis Oncol, 2024, 8(1):52
iScience, 2024, 27(1):108667
S1782 Azacitidine (5-Azacytidine) Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.
Nat Commun, 2024, 15(1):1750
Cell Rep Med, 2024, 5(2):101416
iScience, 2024, 27(2):109011
S2250 EGCG ((-)-Epigallocatechin Gallate) EGCG ((-)-Epigallocatechin Gallate) 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.
Journal of Functional Foods, 2024, 105977
Cell Rep Med, 2023, 4(5):101026
Transl Oncol, 2023, 35:101712
S2821 RG108 RG108 (N-Phthalyl-L-tryptophan) is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, does not cause trapping of covalent enzymes.
Neural Regeneration Research, 2024, 19(10):p 2229-2239
Hereditas, 2023, 160(1):18
Cell Stem Cell, 2022, 29(8):1229-1245.e7
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.
Gastroenterology, 2024, S0016-5085(24)00062-3
Cancer Cell, 2023, 41(1):196-209.e5
Nat Commun, 2022, 13(1):6226
S7276 SGI-1027 SGI-1027 (DNA Methyltransferase Inhibitor II) 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.
Int J Biol Sci, 2022, 18(11):4372-4387
Cancers (Basel), 2022, 14(19)4883
Head Neck, 2022, 44(5):1192-1205
S7113 Zebularine (NSC 309132) Zebularine (NSC 309132, 4-Deoxyuridine) 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.
Leukemia, 2022, 10.1038/s41375-022-01746-3
J Transl Med, 2022, 20(1):383
Plant Physiol, 2022, 190(2):1490-1505
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).
Nutrients, 2023, 15(16)3630
Nutrients, 2023, 15(16)3630
Cell Death Dis, 2021, 12(2):188
S6682 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.
Cell Commun Signal, 2024, 22(1):95
Neural Regeneration Research, 2024, 19(10):p 2229-2239
Int J Mol Sci, 2023, 24(15)12455
S8812 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.
Nat Med, 2019, 25(7):1073-1081
E1046 GSK3685032 GSK3685032 is a non-time-dependent, highly selective enzymatic inhibitor of DNA methyltransferase (DNMT1) with IC50 of 0.036 μM, and over 2500-fold more selective than DNMT3A/3L and DNMT3B/3L.
Nat Commun, 2023, 14(1):3966
S4771 β-thujaplicin β-Thujaplicin (β-TH, Hinokitiol, 4-Isopropyltropolone) 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.
Invest New Drugs, 2022, 10.1007/s10637-022-01229-3
S3543 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.
S4294 Procainamide HCl Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.
S2477 2'-Deoxy-5-Fluorocytidine 2'-Deoxy-5-fluorocytidine (5-fluoro-2(')-deoxycytidine, FCdR), a pyrimidine analog, is a DNA methyltransferase (DMNT) inhibitor currently in clinical trials for solid tumors.
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.
Cell Rep Med, 2024, 5(2):101416
NPJ Precis Oncol, 2024, 8(1):52
iScience, 2024, 27(1):108667
S1782 Azacitidine (5-Azacytidine) Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.
Nat Commun, 2024, 15(1):1750
Cell Rep Med, 2024, 5(2):101416
iScience, 2024, 27(2):109011
S2250 EGCG ((-)-Epigallocatechin Gallate) EGCG ((-)-Epigallocatechin Gallate) 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.
Journal of Functional Foods, 2024, 105977
Cell Rep Med, 2023, 4(5):101026
Transl Oncol, 2023, 35:101712
S2821 RG108 RG108 (N-Phthalyl-L-tryptophan) is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, does not cause trapping of covalent enzymes.
Neural Regeneration Research, 2024, 19(10):p 2229-2239
Hereditas, 2023, 160(1):18
Cell Stem Cell, 2022, 29(8):1229-1245.e7
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.
Gastroenterology, 2024, S0016-5085(24)00062-3
Cancer Cell, 2023, 41(1):196-209.e5
Nat Commun, 2022, 13(1):6226
S7276 SGI-1027 SGI-1027 (DNA Methyltransferase Inhibitor II) 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.
Int J Biol Sci, 2022, 18(11):4372-4387
Cancers (Basel), 2022, 14(19)4883
Head Neck, 2022, 44(5):1192-1205
S7113 Zebularine (NSC 309132) Zebularine (NSC 309132, 4-Deoxyuridine) 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.
Leukemia, 2022, 10.1038/s41375-022-01746-3
J Transl Med, 2022, 20(1):383
Plant Physiol, 2022, 190(2):1490-1505
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).
Nutrients, 2023, 15(16)3630
Nutrients, 2023, 15(16)3630
Cell Death Dis, 2021, 12(2):188
S6682 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.
Cell Commun Signal, 2024, 22(1):95
Neural Regeneration Research, 2024, 19(10):p 2229-2239
Int J Mol Sci, 2023, 24(15)12455
S8812 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.
Nat Med, 2019, 25(7):1073-1081
E1046 GSK3685032 GSK3685032 is a non-time-dependent, highly selective enzymatic inhibitor of DNA methyltransferase (DNMT1) with IC50 of 0.036 μM, and over 2500-fold more selective than DNMT3A/3L and DNMT3B/3L.
Nat Commun, 2023, 14(1):3966
S4771 β-thujaplicin β-Thujaplicin (β-TH, Hinokitiol, 4-Isopropyltropolone) 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.
Invest New Drugs, 2022, 10.1007/s10637-022-01229-3
S3543 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.
S4294 Procainamide HCl Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.
S2477 2'-Deoxy-5-Fluorocytidine 2'-Deoxy-5-fluorocytidine (5-fluoro-2(')-deoxycytidine, FCdR), a pyrimidine analog, is a DNA methyltransferase (DMNT) inhibitor currently in clinical trials for solid tumors.

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Tags: DNA Methyltransferase inhibitor|DNA Methyltransferase agonist|DNA Methyltransferase activator|DNA Methyltransferase inducer|DNA Methyltransferase antagonist|DNA Methyltransferase signaling pathway|DNA Methyltransferase assay kit