DNAメチルトランスフェラーゼ

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1200	Decitabine (NSC 127716)	10 mg/mL	45 mg/mL	''''<1 mg/mL
S1782	Azacitidine (5-Azacytidine)	<1 mg/mL	48 mg/mL	''<1 mg/mL
S2821	RG108	<1 mg/mL	67 mg/mL	'67 mg/mL
S7113	Zebularine (NSC 309132)	46 mg/mL	46 mg/mL	''<1 mg/mL
S1774	Thioguanine (NSC 752)	<1 mg/mL	9 mg/mL	'''<1 mg/mL
S7276	SGI-1027	<1 mg/mL	92 mg/mL	<1 mg/mL
S3957	Gamma-Oryzanol	-1 mg/mL	100 mg/mL	-1 mg/mL
S2250	(-)-Epigallocatechin Gallate	23 mg/mL	72 mg/mL	83 mg/mL
S6682	Bobcat339 hydrochloride	<1 mg/mL	<1 mg/mL	<1 mg/mL
S8812	CM272	<1 mg/mL	96 mg/mL	96 mg/mL
S4771	β-thujaplicin	-1 mg/mL	32 mg/mL	-1 mg/mL
S4294	Procainamide HCl	54 mg/mL	54 mg/mL	54 mg/mL
S2477	2'-Deoxy-5-Fluorocytidine	12 mg/mL	49 mg/mL	'<1 mg/mL

亜型選択性的な製品

DNA Methyltransferase製品

All (13) DNA Methyltransferase阻害剤(13)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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.	Cancer Lett, 2021, 507:26-38 Cell Death Dis, 2021, 12(6):532 Cell Death Discov, 2021, 7(1):90	(A) and (B) SW1116 and LOVO cells were plated, treated for 48 h with decitabine (DAC) and gefitinib (GEF) either alone or in combination, and the expression levels of AKT, mTOR, S6K, and phosphorylation were determined by Western blot analysis as described under Methods. Expression of β-actin served as a loading control. The data are representative of three independent experiments.
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.	J Hematol Oncol, 2021, 14(1):70 Cancers (Basel), 2021, 13(2)E259 Cell Death Dis, 2021, 12(6):570	R-2HG treatment or chemotherapeutic treatment, especially their combinations, decrease MYC levels in leukemic cells (using MONOMAC-6 as a representative). AZA:Azacitidine.
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.	Cell Biol Toxicol, 2021, 10.1007/s10565-021-09596-y Elife, 2020, 30;9. pii: e51317 Anal Chim Acta, 2020, 1103:164-173	The inhibition effect of RG108 on M.SssI MTase activity.
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.	Pain, 2020, 161(1):96-108 J Neuroendocrinol, 2020, 32(2):e12819 Plant Cell, 2018, 30(7):1387-1403	(A) Zebularine treatment suppresses fibre development in vitro. This figure shows that 0 day post anthesis (DPA) ovules cultured for 10 days exhibit different fibre lengths. Different concentrations of zebularine (20, 40 and 80 μM) were applied.
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.	Biosci Rep, 2021, BSR20203890 Front Oncol, 2020, 10:524922 Cancer Cell Int, 2020, 19;20:58
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.	J Med Chem, 2020, 31 Cancer Sci, 2020, 112(1):133-143 Cell Mol Biol Lett, 2019, 24:10	Following the incubation of the unmethylated DNA probe with DNMTase in the presence of spotted DNMTIs, Cy5 intensity values were measured before ( I₀ ) and after ( I₃₀ ) of endonuclease cleavage. Each data set was normalized to the initial fluorescence signal within the corresponding block and the resulting ratio describes the net CpG sites remained uncleaved (盨.D., n = 64). The red line represents the inhibitory threshold determined as two standard deviations below the averaged 'unspotted' ratio. On-chip visualization of the corresponding remaining Cy5 signal is placed on the bottom of each column.
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.	Cell Death Dis, 2021, 12(2):188
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.	Front Pharmacol, 2021, 12:628526 Molecules, 2021, 26(5)1210 Odontology, 2021, 10.1007/s10266-021-00597-1
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
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.
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.
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.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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.	Cancer Lett, 2021, 507:26-38 Cell Death Dis, 2021, 12(6):532 Cell Death Discov, 2021, 7(1):90	(A) and (B) SW1116 and LOVO cells were plated, treated for 48 h with decitabine (DAC) and gefitinib (GEF) either alone or in combination, and the expression levels of AKT, mTOR, S6K, and phosphorylation were determined by Western blot analysis as described under Methods. Expression of β-actin served as a loading control. The data are representative of three independent experiments.
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.	J Hematol Oncol, 2021, 14(1):70 Cancers (Basel), 2021, 13(2)E259 Cell Death Dis, 2021, 12(6):570	R-2HG treatment or chemotherapeutic treatment, especially their combinations, decrease MYC levels in leukemic cells (using MONOMAC-6 as a representative). AZA:Azacitidine.
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.	Cell Biol Toxicol, 2021, 10.1007/s10565-021-09596-y Elife, 2020, 30;9. pii: e51317 Anal Chim Acta, 2020, 1103:164-173	The inhibition effect of RG108 on M.SssI MTase activity.
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.	Pain, 2020, 161(1):96-108 J Neuroendocrinol, 2020, 32(2):e12819 Plant Cell, 2018, 30(7):1387-1403	(A) Zebularine treatment suppresses fibre development in vitro. This figure shows that 0 day post anthesis (DPA) ovules cultured for 10 days exhibit different fibre lengths. Different concentrations of zebularine (20, 40 and 80 μM) were applied.
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.	Biosci Rep, 2021, BSR20203890 Front Oncol, 2020, 10:524922 Cancer Cell Int, 2020, 19;20:58
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.	J Med Chem, 2020, 31 Cancer Sci, 2020, 112(1):133-143 Cell Mol Biol Lett, 2019, 24:10	Following the incubation of the unmethylated DNA probe with DNMTase in the presence of spotted DNMTIs, Cy5 intensity values were measured before ( I₀ ) and after ( I₃₀ ) of endonuclease cleavage. Each data set was normalized to the initial fluorescence signal within the corresponding block and the resulting ratio describes the net CpG sites remained uncleaved (盨.D., n = 64). The red line represents the inhibitory threshold determined as two standard deviations below the averaged 'unspotted' ratio. On-chip visualization of the corresponding remaining Cy5 signal is placed on the bottom of each column.
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.	Cell Death Dis, 2021, 12(2):188
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.	Front Pharmacol, 2021, 12:628526 Molecules, 2021, 26(5)1210 Odontology, 2021, 10.1007/s10266-021-00597-1
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
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.
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.
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.