DNA Methyltransferase

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DNA Methyltransferase製品

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  • DNA Methyltransferase阻害剤 (15)
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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
Biochem Pharmacol, 2024, S0006-2952(24)00048-0
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.
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.
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, 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
Biochem Pharmacol, 2024, S0006-2952(24)00048-0
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.
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.
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, 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.

DNA Methyltransferase阻害剤の選択性比較

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