DNMT
Three DNA methyltransferases (DNMTs), DNMT1, DNMT3a and DNMT3b, catalyze the transfer of a methyl group from S-adenosyl-L-methionine (SAM or AdoMet) to the C5 position of cytosine. DNMT1 is responsible for methylating hemimethylated DNA and thus DNA methylation maintenance, whereas DNMT3a and DNMT3b are involved in de novo DNA methylation, but they can also participate in methylation maintenance. DNMT3a has two different isoforms, and DNMT3b has more than 30 isoforms. DNA methylation profile can be altered leading to DNA instability and triggering diseases such as cancer. In tumorigenesis, methylation in the promoter regions of some genes—such as tumor suppressor genes (TSGs) involved in cellular cycle (e.g., cyclin-dependent kinase (CDK) inhibitors, retinoblastoma protein (RB)), maintenance of genome integrity (e.g., TP53, breast cancer 1 (BRCA1), O6-methylguanine DNA methyltransferase (06-MGMT), mutL homolog 1 (hMLH1)), apoptosis (e.g., caspase 8, death-associated protein kinase (DAPK), migration process (e.g., E-cadherin (CDH1), metalloproteinase inhibitor 3 (TIMP-3)), and those involved in the response to growth factors (phosphatase and tensin homolog (PTEN), estrogen receptor (ER)) leads to their silencing.
References
1.Omar Castillo-Aguilera,et al. Biomolecules. 2017 Mar; 7(1): 3.
References
1.Omar Castillo-Aguilera,et al. Biomolecules. 2017 Mar; 7(1): 3.
Chromatin/Epigenetic
DNMT
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SGI-110
产品货号 : M16656
cas no: 929901-49-5
一种新型 DNA 低甲基化二核苷酸,可抑制 DNA 甲基转移酶 (DNMT)。 -
DC_05
产品货号 : M16429
cas no: 890643-16-0
DC_05 是一种选择性非核苷 DNA 甲基转移酶 DNMT1 抑制剂,IC50 为 10.3 uM。 -
DC_517
产品货号 : M14673
cas no: 500017-70-9
DC_05 是一种有效的、选择性的、非核苷 DNA 甲基转移酶 DNMT1 抑制剂,IC50 为 1.7 uM。 -
RG108
产品货号 : M14614
cas no: 48208-26-0
RG108 是一种 DNA 甲基转移酶抑制剂,在无细胞测定中 IC50 为 115 nM,不会导致共价酶的捕获。 -
Zebularine
产品货号 : M14269
cas no: 3690-10-6
Zebularine 是一种 DNA 甲基化抑制剂,可与 DNA 甲基转移酶形成共价复合物,还可抑制胞苷脱氨酶,在无细胞测定中 Ki 为 2 μM。