Home Epigenetics DNA Methyltransferase

DNA Methyltransferase Inhibitors

Other Epigenetics Related Inhibitors

Histone Methyltransferase BET p300/CBP Histone Demethylase Histone Acetyltransferase MicroRNA NSD EZH1 RNA Methyltransferase SF3B

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.
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
Verified customer review of RG108 (N-Phthalyl-L-Tryptophan)
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
Verified customer review of SGI-1027
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
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

Signaling Pathway Map