| S8812 |
CM272
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CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. This compound prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death.
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Hepatol Commun, 2024, 8(2)e0378
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Nat Med, 2019, 25(7):1073-1081
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| E4795 |
Bobcat339
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Bobcat339 is a cytosine-based small molecule inhibitor of TET enzyme with IC50 of 33 μM and 73 μM for TET1 and TET2, respectively, reducing DNA 5hmC levels in hippocampal neurons. It is useful in epigenetics research and a potential starting point for therapeutics targeting DNA methylation and gene transcription.
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Biomater Res, 2025, 29:0229
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| E1556 |
GSK-3484862
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GSK-3484862 is a non-covalent, potent and selective inhibitor of DNMT1 with an IC50 of 0.23 μM. It demonstrates efficacy in acute myeloid leukemia.
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| S3543 |
DC-05
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DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 10.3 μM and 1.09 μM, respectively.
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| S2477 |
2'-Deoxy-5-Fluorocytidine
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2'-Deoxy-5-fluorocytidine (5-fluoro-2(')-deoxycytidine, FCdR), a pyrimidine analog, is a DNA methyltransferase (DMNT) inhibitor currently in clinical trials for solid tumors.
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| S2250 |
EGCG ((-)-Epigallocatechin Gallate)
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EGCG ((-)-Epigallocatechin Gallate) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.
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Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0694
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Cell Rep, 2025, 44(6):115799
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Front Pharmacol, 2024, 15:1403424
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| S4294 |
Procainamide HCl
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Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.
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Analytical Chemistry, January 12, 2024, 1547-1555
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J Immunother Cancer, 2024, 12(11)e009805
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Journal for ImmunoTherapy of Cancer, 2024, e009805
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