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) |
|
Arginine Methyltransferase (PRMT) |
|
|
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 | |
|---|---|---|---|---|
| 3562 | ML 324 | Inhibitor of JMJD2 histone demethylase | €90.00 | |
| 2081 | ML 324 dihydrochloride | Inhibitor of JMJD2 histone demethylase | €90.00 | |
| 2733 | ML329 | Inhibitor of the MITF molecular pathway | €110.00 | |
| 2003 | MLN 8237 | Second generation selective Aurora A inhibitor | €90.00 | |
| 2505 | Mocetinostat | Class I selective HDAC inhibitor with broad spectrum antitumor activity | €80.00 | |
| 3796 | MRTX1719 hydrochloride | Inhibitor of the PRMT5.MTA complex | Inquire | |
| 1803 | MS 275 | Inhibitor of HDAC (1 and 3 Selective) | €60.00 | |
| 3681 | MS023 dihydrochloride | Potent, cell-active, and Type I selective PRMT inhibitor | €90.00 | |
| 3469 | MS1943 trifluoroacetate | First-in-class EZH2 selective degrader; PROTAC | €200.00 | |
| 2359 | Nexturastat A | HDAC6 inhibitor with good selectivity over HDAC1 and HDAC8 | €90.00 | |
| 2928 | Niraparib | Potent, selective, and orally available PARP1/2 inhibitor | €90.00 | |
| 3409 | NKL 22 | HDAC inhibitor | €80.00 | |
| 1370 | NU 1025 | PARP inhibitor | €80.00 | |
| 2792 | NVP-BSK805 | Potent, selective and orally bioavailable JAK2 inhibitor | €125.00 | |
| 3186 | NVS-BPTF-1 | Potent, selective and cell active chemical probe for BPTF | €180.00 | |
| 2651 | OAC2 | Oct4 and Nanog activating compound that enhances reprogramming efficiency | €60.00 | |
| 3329 | ODM-207 | Highly potent, selective and orally active pan-BET inhibitor | €140.00 | |
| 2442 | OF-1 | Potent bromodomain inhibitor (BRPF1 and BRPF2 selective) | €80.00 | |
| 2077 | OG-L002 hydrochloride | Inhibitor of lysine specific demethylase 1 (LSD1 aka KDM1A) | €125.00 | |
| 3583 | OICR-9429 | First-in-class, potent, highly selective and cell-active antagonist of the Wdr5-MLL interaction | €90.00 | |
| 1464 | Olaparib | PARP inhibitor | €50.00 | |
| 2843 | OSS-128167 | Selective SIRT6 inhibitor | €125.00 | |
| 2530 | OTX 015 | Potent inhibitor of BRD2, BRD3, and BRD4 with clear anti-proliferative activity | €110.00 | |
| 3614 | Parthenolide | NF-κB activation inhibitor | €90.00 | |
| 1853 | PCI 34051 | HDAC8 Inhibitor | €90.00 | |
| 3795 | PDD00017273 | First-in-class, selective and cell-active PARG inhibitor | Recently added | €90.00 |
| 2023 | PF 03814735 | ATP-competitive inhibitor of aurora kinase A and B | €120.00 | |
| 2217 | PF 956980 | JAK3 inhibitor; analogue of Axon 1338 and 2072 | €90.00 | |
| 3695 | PF-06821497 | Inhibitor of Histone Lysine Methyltransferase EZH2 | Inquire | |
| 3798 | PF-06855800 | SAM-pocket-binding (SAM competitive) PRMT5 inhibitor | Inquire | |