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DNA Methyltransferase

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All (14)
DNA Methyltransferase Inhibitors (14)
New DNA Methyltransferase Products

Catalog No.	Product Name	Information	Product Use Citations
E1046^New	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.
S1200	Decitabine (NSC 127716)	Decitabine (NSC 127716, Deoxycytidine, Dacogen, 5-aza-2-deoxycytidine, 5-AZA-dC, 5-aza-CdR) 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 Stem Cell, 2022, S1934-5909(22)00010-8 Signal Transduct Target Ther, 2022, 7(1):35 EMBO Mol Med, 2022, 14(2):e14903
S1774	Thioguanine (NSC 752)	Thioguanine (NSC 752, 6-Thioguanine, 2-Amino-6-purinethiol), 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.	Hum Cell, 2022, 10.1007/s13577-022-00671-y Nat Commun, 2021, 12(1):4961 Microbiol Spectr, 2021, 9(3):e0064621
S1782	Azacitidine (5-Azacytidine)	Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.	Cancer Discov, 2022, candisc.1117.2021 Cancer Cell, 2022, 40(3):301-317.e12 Signal Transduct Target Ther, 2022, 7(1):147
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.	Exp Cell Res, 2022, 411(1):113000 Int J Mol Med, 2022, 49(1)11 J Cardiovasc Pharmacol, 2022, 79(5):711-718
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.
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.	Int J Mol Sci, 2022, 23(8)4213 Front Oncol, 2021, 11:773186 Cell Biol Toxicol, 2021, 10.1007/s10565-021-09596-y
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).	Cell Death Dis, 2021, 12(2):188
S4294	Procainamide HCl	Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.
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
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.	Front Neurol, 2021, 12:652882 Cancer Cell Int, 2020, 20:363
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 K_i of 2 μM in a cell-free assay.	Cell Death Dis, 2021, 12(11):1046 Pain, 2020, 161(1):96-108 J Neuroendocrinol, 2020, 32(2):e12819
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.	Head Neck, 2022, 44(5):1192-1205 Oxid Med Cell Longev, 2021, 2021:5550196 J Ethnopharmacol, 2021, 281:114559
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^New	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.
S1200	Decitabine (NSC 127716)	Decitabine (NSC 127716, Deoxycytidine, Dacogen, 5-aza-2-deoxycytidine, 5-AZA-dC, 5-aza-CdR) 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 Stem Cell, 2022, S1934-5909(22)00010-8 Signal Transduct Target Ther, 2022, 7(1):35 EMBO Mol Med, 2022, 14(2):e14903
S1774	Thioguanine (NSC 752)	Thioguanine (NSC 752, 6-Thioguanine, 2-Amino-6-purinethiol), 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.	Hum Cell, 2022, 10.1007/s13577-022-00671-y Nat Commun, 2021, 12(1):4961 Microbiol Spectr, 2021, 9(3):e0064621
S1782	Azacitidine (5-Azacytidine)	Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.	Cancer Discov, 2022, candisc.1117.2021 Cancer Cell, 2022, 40(3):301-317.e12 Signal Transduct Target Ther, 2022, 7(1):147
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.	Exp Cell Res, 2022, 411(1):113000 Int J Mol Med, 2022, 49(1)11 J Cardiovasc Pharmacol, 2022, 79(5):711-718
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.
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.	Int J Mol Sci, 2022, 23(8)4213 Front Oncol, 2021, 11:773186 Cell Biol Toxicol, 2021, 10.1007/s10565-021-09596-y
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).	Cell Death Dis, 2021, 12(2):188
S4294	Procainamide HCl	Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.
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
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.	Front Neurol, 2021, 12:652882 Cancer Cell Int, 2020, 20:363
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 K_i of 2 μM in a cell-free assay.	Cell Death Dis, 2021, 12(11):1046 Pain, 2020, 161(1):96-108 J Neuroendocrinol, 2020, 32(2):e12819
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.	Head Neck, 2022, 44(5):1192-1205 Oxid Med Cell Longev, 2021, 2021:5550196 J Ethnopharmacol, 2021, 281:114559
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^New	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.