Epigenetics
Epigenetics is typically defined as the study of heritable changes in gene expression that are not due to changes in DNA sequence. Epigenetic modifications of chromatin have been shown to play a major role in cancer onset and development. Acetylation and methylation are the most-studied chromatin marks, having fundamental functions in the epigenetic regulation of gene expression[1],[2].
Epigenetic modification of histones is a reversible process. Histone acetyltransferases (HATs) are the enzymes responsible for the introduction of acetyl groups on histones, whereas methyl groups can be introduced both on DNA and histones by DNA methyltransferases (DNMTs) and histone methyltransferases (HMTs)[3]. The removal of methyl and acetyl groups is enzymatically mediated by the action of histone demethylases (HDMs) and histone deacetylases (HDACs), respectively. In turn, epigenetic marks can be recognized by and bound to specific protein domains, such as bromodomain and malignant brain tumor (MBT). These complexes are important intermediates in the epigenetic regulation of gene expression[4].
Axon Medchem offers a wide selection of bioactive small molecules to modulate epigenetic mechanisms, serving researchers in their objective to investigate biological consequences of chromatin modifications and develop new drugs for cancer treatment.
Epigenetic products Library
For your convenience, you can order a library of all of our Epigenetics related products. Make your personal library by cherry picking products of your interest from our comprehensive list (125 products), or order all together not to miss any. The libraries will be shipped as 10 mM solutions (in DMSO, 250 µL of each selected Axon Ligand™) on a 96-well microtiter plate with a clear map of its contents.
Simply download our comprehensive list of epigenetics products below (Microsoft Excel (.xls)), check the products to be included, and return your list to order the library of your preference.
 Axon Ligands™ - Epigenetics Library.xls |
Modifiers of Histone
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Histone Demethylase (LSD/Jumonji C) |
Histone Deacetylase (HDAC) |
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SET domain lysine Methyltransferase (G9a/EZH2) |
Histone Deacetylase (SIRT) |
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Arginine Methyltransferase (PRMT) |
|
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DNA Methyltransferase (DNMT) |
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Recognition of modified Histone
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Recognition of Acetylated Lysine (Bromodomains) |
Recognition of Metylated Lysine (Kme/MBT) |
[1] Epigenetics in Cancer. Manel Esteller.N Engl J Med 2008; 358, 1148-1159.
[2] Epigenetic protein families: a new frontier for drug discovery. CH Arrowsmith et al. Nature 2012, 11, 384-400.
[3] Histone acetyltransferases as emerging drug targets. FJ Dekker and HJ Haisma. Drug Discov. Today 2009, 14(19-20), 942-948.
[4] Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family. Filippakopoulos, P. et al. Cell 2012, 149, 214-231
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| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2765 | CPTH2 | HAT inhibitor (Gcn5p specific) | €125.00 | |
| 2305 | CX 6258 hydrochloride | Pim kinase inhibitor | €99.00 | |
| 3038 | CXD101 | HDAC inhibitor (1, 2, 3 Selective) | €125.00 | |
| 1681 | CYT 387 | JAK1 and JAK2 inhibitor | €90.00 | |
| 3861 | Decernotinib | Potent and selective,orally bioavailable Janus kinase 3 (JAK3) inhibitor | Recently added | Inquire |
| 1590 | Decitabine | DNA methyltransferase inhibitor | €85.00 | |
| 1977 | DMOG | Cell-permeable HIF-PHD inhibitor with pro-angiogenic and -osteogenic properties | €65.00 | |
| 1268 | DR 2313 | PARP inhibitor | €90.00 | |
| 3398 | E7449 mesylate | Potent, brain penetrable and orally bioavailable dual inhibitor of PARP1/2 and TNKS1/2 | €110.00 | |
| 3424 | Ebselen | Glutathione peroxidase mimic | €60.00 | |
| 2701 | EED226 | Potent, selective and orally bioavailable PRC2 inhibitor | €90.00 | |
| 2568 | EML 425 | Potent reversible dual inhibitor of CBP and p300 (HAT/KAT3) | €95.00 | |
| 2737 | EN460 | Inhibitor of endoplasmic reticulum oxidation 1 (ERO1) | €95.00 | |
| 3674 | Ena21 hydrochloride | Selective and competitive ALKBH5 inhibitor | €110.00 | |
| 2831 | EPZ 015666 | Potent, selective and orally available inhibitor of PRMT5 | €125.00 | |
| 2227 | EPZ 6438 | Inhibitor of Histone Lysine Methyltransferase EZH2 | €105.00 | |
| 2384 | FDI 6 | Inhibitor of the Forkhead box protein M1 (FOXM1) | €99.00 | |
| 2570 | FG-2216 | Orally active HIF-PHD inhibitor that increases plasma EPO levels in vivo | €80.00 | |
| 2277 | FLI 06 | Notch signaling inhibitor that acts early in the secretory pathway | €95.00 | |
| 2959 | FM19G11 | Potent HIFα inhibitor | €95.00 | |
| 2208 | Gallic acid | Multi-affinity drug. Antioxidant. | €50.00 | |
| 2885 | GeA-69 | Selective allosteric and cell-active PARP14 MD2 inhibitor | €95.00 | |
| 2140 | GSK 126 | Inhibitor of Histone Lysine Methyltransferase EZH2 | €75.00 | |
| 2410 | GSK 5959 | Potent, cell permeable inhibitor of BRPF1 bromodomain | €135.00 | |
| 1934 | GSK J1 | Histone demethylase JMJD3/UTX inhibitor | €105.00 | |
| 1933 | GSK J4 | Histone demethylase JMJD3/UTX inhibitor | €105.00 | |
| 2375 | GSK-LSD1 | Irreversible inhibitor of the KDM1 family histone demethylase LSD1 | €100.00 | |
| 3750 | GSK3326595 | Orally active, potent, selective, SAM uncompetitive, peptide competitive, slow binding inhibitor of protein arginine methyltransferase 5 (PRMT5) | Inquire | |
| 3757 | GSK3685032 hydrochloride | Potent first-in-class DNMT1-selective inhibitor | Inquire | |
| 1645 | HDAC6 inhibitor ISOX | HDAC6 Inhibitor | €110.00 | |