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DNA Methyltransferase

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TET DNMT1 DNMT3

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DNA Methyltransferase Products

All (16)
DNA Methyltransferase Inhibitors (16)
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.	Nat Commun, 2024, 15(1):7360 Cell Rep Med, 2024, 5(2):101416 J Immunother Cancer, 2024, 12(11)e009805
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 Hematol Oncol, 2024, 17(1):85 Nat Commun, 2024, 15(1):7360 Nat Commun, 2024, 15(1):4739
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 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 Cancer Cell, 2023, 41(1):196-209.e5
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
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.
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.	Nat Commun, 2024, 15(1):7360 Cell Rep Med, 2024, 5(2):101416 J Immunother Cancer, 2024, 12(11)e009805
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 Hematol Oncol, 2024, 17(1):85 Nat Commun, 2024, 15(1):7360 Nat Commun, 2024, 15(1):4739
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 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 Cancer Cell, 2023, 41(1):196-209.e5
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
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.
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.

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