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Antioxidant, antiangiogenic, antitumor agent
(-)-Epigallocatechin gallate is a potent anti-oxidant polyphenol flavonoid isolated from green tea.- Siyu Zhu, .et al. , Toxicol Appl Pharmacol, 2025, Jul:500:117380 PMID: 40348029
- Grace Northrop, .et al. , Food Funct, 2022, Apr 4;13(7):3894-3904 PMID: 35285840
- Wafa Dridi, .et al. , Carbohydr Polym, 2021, 274:118670 PMID: 34702486
- A S D'Costa, .et al. , Food Chem, 2020, Oct 1;341(Pt 2):128256 PMID: 33035827
- Fenteany G, .et al. , Sci Rep, 2019, Sep 5;9(1):12801 PMID: 31488855
- LiliSun, .et al. , Nutrition, 2019, pii:S0899-9007(18)31140-7
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DNMT inhibitor
Azacitidine is a chemical analogue of the cytosine nucleoside used in DNA and RNA that is mainly used in the treatment of myelodysplastic syndrome (MDS).- Nageswara Rao Reddy, .et al. , Bioanalysis, 2022, Mar;14(5):253-266 PMID: 35172610
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DNA Methyltransferase Inhibitors
Decitabine is a hypomethylating agent.It hypomethylates DNA by inhibiting DNA methyltransferase.- Tianxing Ying, .et al. , Cancers (Basel), 2022, Dec 30;15(1):243 PMID: 36612238
- Borbala Szabo, .et al. , J Clin Endocrinol Metab, 2022, Sep 5;dgac496 PMID: 36059148
- Sangni Qian, .et al. , Clin Epigenetics, 2022, Sep 5;14(1):111 PMID: 36064442
- Borb??la Szab??, .et al. , J Clin Endocrinol Metab, 2020, Jun 1;105(6):dgaa156 PMID: 32232382
- Bracha Shraibman, .et al. , Mol Cell Proteomics, 2016, Sep; 15(9): 3058-3070 PMID: 27412690
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MGMT inhibitor
O6BTG-octylglucoside is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells. -
DNA methyltransferase inhibitor
Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor. -
DNMT inhibitor
SGI-110 is a second generation DNA-hypomethyating agent.- Lise Brault, .et al. , EMBO Mol Med, 2025, Aug 29 PMID: 40883610
- Sho Sato, .et al. , Sci Rep, 2023, Jan 27;13(1):1537 PMID: 36707610
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MGMT inhibitor
Lomeguatrib is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase. -
MGMT inhibitor
O6-Benzylguanine is an effective substrate and efficient inactivator of DNA alkyltransferase. O6-Benzylguanine is an inhibitor of MGMT. -
Sodium channel blocker/DNMT inhibitor
Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor. -
antineoplastic activity
Guadecitabine, aslo known as SGI-110, is a dinucleotide antimetabolite of a decitabine linked via phosphodiester bond to a guanosine, with potential antineoplastic activity. - β-Thujaplicin 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.
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DNMT inhibitor
MC3343 is a DNMT inhibitor (EC50: 5.7 μM) and potent DNA binder that inhibits tumor proliferation by arresting osteosarcoma (OS) cells in the G1 or G2/M phases. It promotes osteoblastic differentiation by specifically reactivating genes involved in this physiological process. -
NSUN2 inhibitor
MY-1B is a covalent inhibitor of the RNA methyltransferase NSUN2 (IC50: 1.3 μM), stereoselectively targeting active-site cysteine residues (C271). It also covalently binds to PSME1, disrupting the proteasome regulatory complex and downregulating specific MHC-I subtype presentation. -
5-Methyldeoxycytidine
5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases, including mammalian 5-C-MTase, and binds to DNA in a manner dependent on DNA stem-loop structure formation. It directs de novo DNA methylation by serving as a methylation mark, promoting methylation of adjacent CpG sites in single-stranded DNA via cis-acting mechanisms. 5mdC regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, influencing chromatin condensation and gene expression. In plant cells, its distribution correlates with cell proliferation and differentiation stages, with lower methylation levels in proliferating cells and higher levels in differentiated cells. -
TET2 inhibitor
TFMB-(S)-2-HG is a potent inhibitor of TET2 and EglN prolyl hydroxylases. It downregulates Wnt3a and intranuclear β-catenin protein expression, and inhibits osteogenic differentiation of cells. TFMB-(S)-2-HG shows potential for research in acute myeloid leukemia (AML). -
HDAC1/DNA Methyltransferase Inhibitor
Psammaplin A, a marine-derived metabolite, is a potent inhibitor of HDAC1 (IC50: 45 nM), DNA methyltransferases (IC50: 18.6 nM), and aminopeptidase N (IC50: 18 μM). It also suppresses DNA topoisomerase and farnesyl protein transferase activities. As a PPARγ activator, Psammaplin A induces apoptosis and exhibits antitumor, anti-inflammatory, and anti-angiogenic properties. Additionally, it demonstrates antibacterial activity against Gram-positive bacteria by inhibiting DNA synthesis and DNA -
DNMT inhibitor
5-Fluoro-2'-deoxycytidine (FdCyd) is a fluoropyrimidine nucleoside analogue that functions as a DNA methyltransferase (DNMT) inhibitor. It also serves as a tumor-selective prodrug of 5-fluoro-2′-dUMP, a thymidylate synthase inhibitor. FdCyd induces cell cycle arrest in tumor cells by activating the DNA damage response and exhibits potent anti-tumor activity, making it a promising agent in epigenetic and chemotherapeutic cancer research. -
DNMT1 inhibitor
DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor with an IC₅₀ of 10.3 μM and a binding affinity (K\_d) of 1.09 μM. It interferes with DNMT1-mediated DNA methylation, making it a useful compound for studying epigenetic regulation and exploring potential therapeutic applications in diseases involving aberrant DNA methylation. -
TET inhibitor
Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET (ten-eleven translocation) enzymes, with IC₅₀ values of 33 μM for TET1 and 73 μM for TET2. By inhibiting TET-mediated DNA demethylation, it modulates epigenetic regulation and gene transcription. Bobcat339 hydrochloride is a valuable tool in epigenetics research and serves as a potential lead compound for developing therapeutics targeting DNA methylation-related diseases. -
DNMT1 inhibitor
GSK-3484862 is a non-covalent and selective inhibitor of DNA methyltransferase 1 (DNMT1). It effectively induces DNA hypomethylation, making it a promising agent for cancer therapy. In murine embryonic stem cells, GSK-3484862 mediates robust and targeted demethylation with minimal off-target toxicity, supporting its potential for epigenetic reprogramming and therapeutic applications. -
DNMT1 inhibitor
GSK-3685032 is a first-in-class, reversible, non-time-dependent, and noncovalent inhibitor that selectively targets DNA methyltransferase 1 (DNMT1), with an IC₅₀ of 0.036 μM. It induces robust DNA demethylation, leading to transcriptional activation and inhibition of cancer cell growth, making it a promising candidate for epigenetic therapy in oncology. -
DNA Methyltransferase Inhibitor
RSC133 is a dual epigenetic modulator that inhibits both histone deacetylases (HDACs) and DNA methyltransferases (DNMTs). It effectively enhances the reprogramming of human somatic cells into induced pluripotent stem cells (iPSCs) and supports the maintenance of pluripotency by promoting an undifferentiated state. RSC133 is a valuable tool for stem cell research and epigenetic reprogramming studies. -
Antiepileptic Agent
Levetiracetam is an antiepileptic agent that targets the synaptic vesicle protein SV2A. It has been shown to enhance the effects of Temozolomide on glioblastoma stem cell proliferation and apoptosis. Additionally, Levetiracetam modulates histone deacetylase (HDAC) levels, leading to the silencing of MGMT, which further improves the efficacy of Temozolomide. This compound serves as a valuable chemosensitizer in cancer research applications. -
DNA Methyltransferase Inhibitor
γ-Oryzanol is an effective inhibitor of DNA methyltransferases (DNMTs) with a primary focus on DNMT1 and DNMT3a. It demonstrates significant inhibitory activity, with an IC50 of 3.2 μM for DNMT1 and 22.3 μM for DNMT3a. This compound has important implications for epigenetic research and may be useful in studies exploring gene expression regulation and potential therapeutic applications in cancer and other diseases associated with aberrant DNA methylation. -
DNMT/HDAC Inhibitor
DNMT/HDAC-IN-2 is a dual inhibitor of DNA methyltransferase (DNMT) and histone deacetylases (HDAC), exhibiting IC50 values of 365 nM for DNMT1, 0.2 nM for HDAC1, and 8.91 nM for HDAC6. This compound effectively inhibits the proliferation of breast cancer cells and demonstrates significant anti-tumor activity in xenograft and transgenic mouse models of breast cancer. DNMT/HDAC-IN-2 serves as a valuable tool for investigating epigenetic modification in breast cancer research. -
DNMT And HDAC Aual Inhibitor
DNMT/HDAC-IN-1 is a dual inhibitor targeting DNA methyltransferases (DNMT) and histone deacetylases (HDACs), demonstrating IC50 values of 56.84 nM for HDAC1 and 17.39 nM for HDAC6. This compound induces apoptosis in tumor cells and is valuable for cancer research applications, providing insights into the mechanisms of epigenetic regulation in malignancies. Its role in modulating both DNMT and HDAC activities makes it a significant tool for investigating therapeutic strategies in oncology. -
G9a/DNMT Inhibitor
CM-579 trihydrochloride is a reversible dual inhibitor targeting G9a and DNMT, demonstrating IC50 values of 16 nM and 32 nM, respectively. This compound exhibits significant in vitro cellular activity across various cancer cell types, making it a valuable tool for epigenetic research and cancer therapeutics. Its ability to modulate histone methylation and DNA methylation positions CM-579 trihydrochloride as a key reagent for studies investigating the role of these enzymes in oncogenesis and potential treatment strategies. -
DNMT Inhibitor
DNMT1-IN-5 is a selective inhibitor targeting DNA methyltransferases DNMT1 and DNMT3A, with IC50 values of 2.42 μM and 14.4 μM, respectively. This compound demonstrates significant antiproliferative activity across various cancer cell lines, exhibiting IC50 values ranging from 0.19 to 2.37 μM in TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226, and HCT116. In addition to inducing cell cycle arrest at the G2/M phase, DNMT1-IN-5 promotes apoptosis in TMD-8 and DOHH2 cells and has shown antitumor efficacy in xenograft mouse models. -
HDAC/DNMT Inhibitor
J208 is a dual inhibitor targeting histone deacetylase (HDAC) and DNA methyltransferase (DNMT). This compound effectively inhibits the proliferation of cancer cells and reduces the migration and invasion of triple-negative breast cancer (TNBC) cells. J208 also induces apoptosis and halts the cell cycle at the G0/G1 phase, while activating innate immune signaling pathways by promoting the expression of endogenous retroviruses (ERVs) in TNBC. It serves as a valuable tool for investigating epigenetic regulation and cancer therapy. -
DNMT3A Inhibitor
(4aS,8aR)-NPD-001 is a potent allosteric inhibitor targeting DNMT3A, disrupting critical protein-protein interactions essential for its activity. This compound demonstrates significant biological activity by inducing apoptosis in acute myeloid leukemia (AML) cell lines and promoting differentiation in various AML cell types, including those harboring the R882 mutation in DNMT3A. Its specific modulation of DNMT3A makes (4aS,8aR)-NPD-001 a valuable tool for research on epigenetic regulation in hematological malignancies. -
DNA Methyltransferase Inhibitor
N-Acetyl-S-geranylgeranyl-L-cysteine is a potent inhibitor of DNA methyltransferases. This compound effectively disrupts beta-2 integrin-induced actin polymerization, demonstrating an IC50 of 45 nM. It serves as a valuable tool in studying epigenetic regulation and cellular signaling pathways related to cancer and other diseases. -
DNA Methyltransferase Inhibitor
DC_517 is a selective inhibitor of DNA methyltransferase 1 (DNMT1), exhibiting an IC50 of 1.7 μM and a Kd of 0.91 μM. This compound effectively modulates DNA methylation patterns, making it a valuable tool for studies related to epigenetic regulation, gene expression, and cancer research. Research applications include exploring the roles of DNMT1 in cellular processes and evaluating potential therapeutic strategies for diseases associated with abnormal DNA methylation. -
DNA Methyltransferase
CpG Methyltransferase is a DNA methyltransferase that specifically targets the C5 position of cytosine nucleotides in unmethylated or hemimethylated double-stranded DNA within a 5’-CpG-3’ context. This enzyme facilitates the addition of a methyl group, which plays a crucial role in gene regulation and epigenetic modification. It is widely utilized in research applications involving DNA methylation studies, gene expression analysis, and the investigation of epigenetic mechanisms in various biological processes. -
DNA Methyltransferase Inhibitor
DNMT-IN-6 is a potent DNA methyltransferase inhibitor targeting DNMT1, DNMT3A, and DNMT3B. It promotes demethylation and restores expression of the TMS1 tumor suppressor gene, leading to apoptosis and G2/M phase cell cycle arrest. Additionally, DNMT-IN-6 disrupts mitochondrial integrity and activates the intrinsic caspase cascade (caspases 3, 7, and 9). This compound demonstrates potential in inhibiting tumor growth and enhancing survival in xenograft models, making it a valuable tool for cancer research, particularly in the study of diffuse large B-cell lymphoma. -
DNA Methyltransferase Inhibitor
2′-Deoxy-5-nitrocytidine is a potent inhibitor of DNA methyltransferase, disrupting the methylation process crucial for gene expression regulation. This compound is primarily utilized in cancer research to investigate its effects on tumorigenesis and cellular differentiation. By modulating DNA methylation patterns, it provides valuable insights into epigenetic modifications and their implications in various malignancies. -
DNA Methyltransferase
HhaI Methyltransferase is a DNA methyltransferase that specifically recognizes the sequence GCGC. This enzyme catalyzes the transfer of a methyl group to cytosine residues within this recognition site, playing a critical role in the regulation of gene expression and genomic stability. It is widely utilized in epigenetic research, DNA methylation studies, and the development of methylation-sensitive tools for molecular biology applications.

