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DNA Methyltransferase

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TET DNMT1 DNMT3

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DNA Methyltransferase Products

All (17)
DNA Methyltransferase Inhibitors (17)
New DNA Methyltransferase Products

Catalog No.	Product Name	Information	Product Use Citations
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.	Biomark Res, 2025, 13(1):17 EMBO Rep, 2025, 10.1038/s44319-025-00385-w Oncogenesis, 2025, 14(1):1
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.	J Mol Cell Cardiol, 2025, 198:45-59 Heliyon, 2025, 11(3):e41948 J Hematol Oncol, 2024, 17(1):85
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.	Front Pharmacol, 2024, 15:1403424 Heliyon, 2024, 10(21):e39933 Biochem Biophys Res Commun, 2024, 736:150907
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 Regen Res, 2024, 19(10):2229-2239 Neural Regeneration Research, 2024, 19(10):p 2229-2239 Hereditas, 2023, 160(1):18
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 Cancers (Basel), 2024, 16(21)3606 BMC Genomics, 2024, 25(1):1030
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.	Eur J Pharm Sci, 2024, 197:106767 Parasites Hosts Dis, 2024, 62(1):98-116 Int J Biol Sci, 2022, 18(11):4372-4387
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.	Insect Mol Biol, 2024, 10.1111/imb.12933 Leukemia, 2022, 10.1038/s41375-022-01746-3 J Transl Med, 2022, 20(1):383
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).	PLoS One, 2024, 19(5):e0302745 Nutrients, 2023, 15(16)3630 Nutrients, 2023, 15(16)3630
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.	Nat Cell Biol, 2024, 10.1038/s41556-024-01475-y Cell Death Dis, 2024, 15(8):617 Cell Commun Signal, 2024, 22(1):95
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.	Hepatol Commun, 2024, 8(2)e0378 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, 2024, 15(1):7360 Nat Commun, 2023, 14(1):3966 GHENT UNIVERSITY, 2022,
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
E1556^New	GSK-3484862	GSK-3484862 is a non-covalent, potent and selective inhibitor of DNMT1 with an IC50 of 0.23 μM. It demonstrates efficacy in acute myeloid leukemia.
E4795^New	Bobcat339	Bobcat339 is a cytosine-based small molecule inhibitor of TET enzyme with IC50 of 33 μM and 73 μM for TET1 and TET2, respectively, reducing DNA 5hmC levels in hippocampal neurons. It is useful in epigenetics research and a potential starting point for therapeutics targeting DNA methylation and gene transcription.
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.	J Immunother Cancer, 2024, 12(11)e009805
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.	Biomark Res, 2025, 13(1):17 EMBO Rep, 2025, 10.1038/s44319-025-00385-w Oncogenesis, 2025, 14(1):1
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.	J Mol Cell Cardiol, 2025, 198:45-59 Heliyon, 2025, 11(3):e41948 J Hematol Oncol, 2024, 17(1):85
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.	Front Pharmacol, 2024, 15:1403424 Heliyon, 2024, 10(21):e39933 Biochem Biophys Res Commun, 2024, 736:150907
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 Regen Res, 2024, 19(10):2229-2239 Neural Regeneration Research, 2024, 19(10):p 2229-2239 Hereditas, 2023, 160(1):18
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 Cancers (Basel), 2024, 16(21)3606 BMC Genomics, 2024, 25(1):1030
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.	Eur J Pharm Sci, 2024, 197:106767 Parasites Hosts Dis, 2024, 62(1):98-116 Int J Biol Sci, 2022, 18(11):4372-4387
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.	Insect Mol Biol, 2024, 10.1111/imb.12933 Leukemia, 2022, 10.1038/s41375-022-01746-3 J Transl Med, 2022, 20(1):383
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).	PLoS One, 2024, 19(5):e0302745 Nutrients, 2023, 15(16)3630 Nutrients, 2023, 15(16)3630
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.	Nat Cell Biol, 2024, 10.1038/s41556-024-01475-y Cell Death Dis, 2024, 15(8):617 Cell Commun Signal, 2024, 22(1):95
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.	Hepatol Commun, 2024, 8(2)e0378 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, 2024, 15(1):7360 Nat Commun, 2023, 14(1):3966 GHENT UNIVERSITY, 2022,
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
E1556^New	GSK-3484862	GSK-3484862 is a non-covalent, potent and selective inhibitor of DNMT1 with an IC50 of 0.23 μM. It demonstrates efficacy in acute myeloid leukemia.
E4795^New	Bobcat339	Bobcat339 is a cytosine-based small molecule inhibitor of TET enzyme with IC50 of 33 μM and 73 μM for TET1 and TET2, respectively, reducing DNA 5hmC levels in hippocampal neurons. It is useful in epigenetics research and a potential starting point for therapeutics targeting DNA methylation and gene transcription.
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.	J Immunother Cancer, 2024, 12(11)e009805
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.
E1556^New	GSK-3484862	GSK-3484862 is a non-covalent, potent and selective inhibitor of DNMT1 with an IC50 of 0.23 μM. It demonstrates efficacy in acute myeloid leukemia.
E4795^New	Bobcat339	Bobcat339 is a cytosine-based small molecule inhibitor of TET enzyme with IC50 of 33 μM and 73 μM for TET1 and TET2, respectively, reducing DNA 5hmC levels in hippocampal neurons. It is useful in epigenetics research and a potential starting point for therapeutics targeting DNA methylation and gene transcription.

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