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 Ki 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. |
-
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
|
|
E1556New |
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 Ki 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. |
- 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
|
|
E1556New |
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. |
|
|