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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.
Nucleic Acids Res, 2026, 54(4)gkag089
Sci Rep, 2026, 16(1)14560
Cancer Res Commun, 2026, 6(3):648-656
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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.
Cell Rep Med, 2026, 7(3):102687
Mol Cancer, 2025, 24(1):154
Cell Rep Med, 2025, S2666-3791(25)00102-8
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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.
Psychopharmacology (Berl), September 13, 2025, Online ahead of print
Cell Reports, March 26, 2025, 115480
Cell Communication and Signaling, February 2, 2024, 95
S2821 RG108 (N-Phthalyl-L-Tryptophan) 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.
J Transl Med, 2025, 23(1):193
Cells, 2025, 14(2)135
Neural Regen Res, 2024, 19(10):2229-2239
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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.
Cell Death & Disease, September 7 2020, 724
Oxidative Medicine and Cellular Longevity, July 19 2021, 5550196
Eur J Pharm Sci, 2024, 197:106767
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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
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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
bioRxiv, 2025, nan
Nat Commun, 2024, 15(1):7360
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
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.
International Journal of Translational Medicine, July 7, 2025, 29
Investigational New Drugs, August 2022, 700-708
International Journal of Translational Medicine, 2025, 29

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