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DNA Methyltransferase Inhibitors

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Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
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.
Cancer Cell, 2025, S1535-6108(25)00223-5
Nat Commun, 2025, 16(1):4451
Cell Rep Med, 2025, S2666-3791(25)00102-8
Verified customer review of Decitabine
S1782 5-Azacytidine (5-Aza, Azacitidine) 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.
Mol Cancer, 2025, 24(1):154
Cell Rep Med, 2025, S2666-3791(25)00102-8
Cell Rep Med, 2025, 6(12):102461
Verified customer review of 5-Azacytidine (5-Aza, Azacitidine)
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.
EMBO Mol Med, 2025, 17(10):2809-2826
Nat Cell Biol, 2024, 10.1038/s41556-024-01475-y
Cell Death Dis, 2024, 15(8):617
S2821 RG108 RG108 (N-Phthalyl-L-tryptophan) is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, and this compound does not cause trapping of covalent enzymes.
J Transl Med, 2025, 23(1):193
Cells, 2025, 14(2)135
Neural Regen Res, 2024, 19(10):2229-2239
Verified customer review of RG108
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.
BMC Microbiol, 2025, 25(1):53
Gastroenterology, 2024, S0016-5085(24)00062-3
iScience, 2024, 27(10):110862
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. This compound 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
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S7113 Zebularine (NSC 309132) Zebularine (NSC 309132, 4-Deoxyuridine) is a DNA methylation inhibitor that forms a covalent complex with DNA methyltransferases; it also inhibits cytidinedeaminase with a 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
Verified customer review of Zebularine (NSC 309132)
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.
NPJ Precis Oncol, 2025, 9(1):62
Nat Commun, 2024, 15(1):7360
Nat Commun, 2023, 14(1):3966
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
Cell Death Dis, 2021, 12(2):188
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. This compound 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

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