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 | |
|---|---|---|---|---|
| 2537 | 1,5-Isoquinolinediol | PARP1 inhibitor and neuroprotective agent | €50.00 | |
| 1496 | 3-Aminobenzamide | Competitive small molecule inhibitor of PARP | €40.00 | |
| 1529 | AG 014699 | PARP1 inhibitor | €60.00 | |
| 3834 | Alantolactone | STAT3 inhibitor; NLRP3 inhibitor | €90.00 | |
| 2241 | AZD2461 | PARP inhibitor with poor P-glycoprotein substrate qualities | €95.00 | |
| 3009 | BRD0539 | Reversible and cell-permeable Cas9 inhibitor | €170.00 | |
| 2699 | CCT251236 | HSF1 stress pathway inhibitor | €130.00 | |
| 1590 | Decitabine | DNA methyltransferase inhibitor | €85.00 | |
| 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 | |
| 2701 | EED226 | Potent, selective and orally bioavailable PRC2 inhibitor | €90.00 | |
| 3674 | Ena21 hydrochloride | Selective and competitive ALKBH5 inhibitor | €110.00 | |
| 2384 | FDI 6 | Inhibitor of the Forkhead box protein M1 (FOXM1) | €99.00 | |
| 2959 | FM19G11 | Potent HIFα inhibitor | €95.00 | |
| 2885 | GeA-69 | Selective allosteric and cell-active PARP14 MD2 inhibitor | €95.00 | |
| 3900 | GSK-3484862 | No-covalent DNMT1-selective inhibitor | Inquire | |
| 3757 | GSK3685032 hydrochloride | Potent first-in-class DNMT1-selective inhibitor | Inquire | |
| 2034 | HIF-2 inhibitor 2 | Allosteric inhibitor of HIF-2 | €95.00 | |
| 2614 | HIF-2a Translation Inhibitor 76 | HIF-2a translation inhibitor that works independent of mTOR | €70.00 | |
| 3417 | IMT1B | First-in-class, potent and highly specific allosteric POLRMT inhibitor | €130.00 | |
| 1566 | Iniparib | PARP inhibitor | €60.00 | |
| 4179 | KU-0058948 | Potent and specific PARP1 inhibitor | €135.00 | |
| 2001 | KU-0058948 hydrochloride | Potent and specific PARP1 inhibitor | €135.00 | |
| 2549 | L67 | Cytotoxic inhibitor of DNA ligase I and III | €90.00 | |
| 2223 | Lomeguatrib | Potent, orally active inhibitor of MGMT | €135.00 | |
| 2480 | LW6 | Inhibitor of HIF-1α stability via MDH2 inhibition and/or binding with CHP1 | €85.00 | |
| 2759 | ME0328 | PARP3/ARTD3 inhibitor | €95.00 | |
| 2733 | ML329 | Inhibitor of the MITF molecular pathway | €110.00 | |
| 2928 | Niraparib | Potent, selective, and orally available PARP1/2 inhibitor | €90.00 | |
| 1370 | NU 1025 | PARP inhibitor | €80.00 | |