DNMT1
DNMT1 (DNA methyltransferase 1) is the principal maintenance DNA methyltransferase that preferentially recognizes hemimethylated CpG sites and preserves DNA methylation patterns during DNA replication, thereby supporting epigenetic inheritance and stable gene regulation[1][2]. Mechanistically, DNMT1 functions within the DNA methylation machinery that maintains chromatin states, transcriptional programs, and genome stability, and its recruitment to newly replicated DNA is coordinated by factors such as UHRF1[1][3]. Through maintenance of CpG methylation, DNMT1 contributes to developmental processes, cellular identity, and long-term repression of transposable elements[1][4]. In disease contexts, aberrant DNMT1 activity is strongly associated with cancer, where sustained DNA methylation can promote silencing of tumor-suppressor genes and support malignant phenotypes[1][5][6]. Experimental studies further demonstrate that selective depletion of DNMT1 induces global and gene-specific demethylation and reactivates silenced tumor-suppressor genes in human cancer cells, highlighting its central role in epigenetic regulation[6]. Compared with the related de novo methyltransferases DNMT3A and DNMT3B, which establish new methylation patterns, DNMT1 primarily propagates existing methylation marks after DNA replication, although recent evidence indicates that DNMT1 can also exhibit context-dependent de novo methylation activity, particularly at retrotransposon loci[4]. For experimental applications, DNMT1 remains a major epigenetic drug target, and both nucleoside-based and emerging selective non-nucleoside inhibitors are widely used to investigate DNA methylation dynamics and therapeutic reprogramming of aberrant epigenetic states[5].
References:
- [1]. Tutucci E, et al. Keeping mRNPs in check during assembly and nuclear export. Nat Rev Mol Cell Biol. 2011 Jun;12(6):377-84. [Content Brief]
- [2]. Rossi M, et al. Eicosapentaenoic acid modulates the synergistic action of CREB1 and ID/E2A family members in the rat pup brain and mouse embryonic stem cells. Biochim Biophys Acta Gene Regul Mech. 2017 Aug;1860(8):870-884. [Content Brief]
- [3]. Wikipedia.
- [4]. Haggerty C, et al. Dnmt1 has de novo activity targeted to transposable elements. Nat Struct Mol Biol. 2021 Jul;28(7):594-603. [Content Brief]
- [5]. Rabezanahary H, et al. Live virus neutralizing antibodies against pre and post Omicron strains in food and retail workers in Québec, Canada. Heliyon. 2024 May 21;10(10):e31026. [Content Brief]
- [6]. Boocock GR, et al. Mutations in SBDS are associated with Shwachman-Diamond syndrome. Nat Genet. 2003 Jan;33(1):97-101. [Content Brief]
All Product Categories
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DNMT1 Related Products (32)
Related Products (32)
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Antibodies (1)
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CM-579
0 ImagesCat. No.: HY-117421CAS No.: 1846570-40-8CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
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MC3817
0 ImagesCat. No.: HY-179409Purity: 99.88%MC3817 is a selective DNMT1 inhibitor. MC3817 inhibits DNMT1 and DNMT3A/3L with IC50s of 0.044 μM and > 10μM, respectively. MC3817 inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage MC3817 elevates cleaved Caspase 3, P53, and γH2AX. MC3817 can be used in non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer and histiocytic lymphoma research.
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MC3817 free base
0 ImagesCat. No.: HY-179409AMC3817 free base is a selective DNMT1 inhibitor. MC3817 free base inhibits DNMT1 and DNMT3A/3L with IC50s of 0.044 μM and > 10μM, respectively. MC3817 free base inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage. MC3817 free base elevates cleaved Caspase 3, P53, and γH2AX. MC3817 free base can be used in non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer and histiocytic lymphoma research.
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DNMT1-IN-3
0 ImagesCat. No.: HY-161694CAS No.: 3025012-68-1DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor.
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DNMT1-IN-5
0 ImagesCat. No.: HY-172217CAS No.: 2982511-19-1DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC50 of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC50s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models.
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GSK-3484862 (GMP)
0 ImagesCat. No.: HY-135146GCAS No.: 2170136-65-7Synonyms: (R)-GSK3482364 (GMP)GSK-3484862 GMP is GSK-3484862 (HY-135146) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma.
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DNMT/HDAC-IN-2
0 ImagesCat. No.: HY-175988CAS No.: 2548725-57-9DNMT/HDAC-IN-2 (Compound Y7) is a DNMT and HDAC inhibitor with IC50 values for DNMT1, HDAC1, and HDAC6 of 365, 0.2, and 8.91 nM respectively. DNMT/HDAC-IN-2 inhibits the proliferation of breast cancer cells. DNMT/HDAC-IN-2 significantly reduces tumor growth in xenografts and transgenic breast cancer mouse models. DNMT/HDAC-IN-2 can be used for the study of breast cancer.
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RG108 (GMP)
0 ImagesCat. No.: HY-13642GCAS No.: 48208-26-0RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
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GSK3830052
0 ImagesCat. No.: HY-183852CAS No.: 2170141-06-5GSK3830052 is a selective DNA methyltransferase 1 (DNMT1) inhibitor. GSK3830052 can be used to study cancer, sickle cell disease, β-thalassemia, and other diseases associated with DNMT1 inhibition.
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DNMT1 Degrader-1
0 ImagesDNMT1 Degrader-1 is a selective DNMT1 degrader with an IC50 of 202.87 nM and a Kd value of 122 nM. As a molecular glue, DNMT1 Degrader-1 forms a ternary complex with DNMT1 and UHRF1, thereby triggering UHRF1-mediated ubiquitination and degradation of DNMT1, and inhibiting the enzymatic activity of DNMT1. DNMT1 Degrader-1 inhibits the proliferation of primary acute myeloid leukemia cells and exerts anti-tumor activity. DNMT1 Degrader-1 can be used for the research of acute myeloid leukemia.
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CM-444
0 ImagesCat. No.: HY-163803CAS No.: 2256079-52-2CM-444 is inhibitor for HDAC (IC50 is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC50 is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models.
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