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 | |
|---|---|---|---|---|
| 1541 | ZM 447439 | Aurora B inhibitor | €85.00 | |
| 2445 | ZLN 024 | Allosteric activator of AMP-activated protein kinase (AMPK) | €90.00 | |
| 1254 | Zebularine | DNA methyltransferase inhibitor | €95.00 | |
| 2674 | YUKA1 | Selective inhibitor of KDM5A demethylase | €125.00 | |
| 2231 | XL 019 | JAK2 inhibitor | €100.00 | |
| 2969 | WM-1119 | Highly potent and selective KAT6A inhibitor | €130.00 | |
| 2411 | WDR5-0103 | Inhibitor of WD40 repeat protein 5 (WDR5) and associated activity of H3K4 HMTase MLL | €90.00 | |
| 1540 | VX 680 | Aurora inhibitor (non-specific) | €60.00 | |
| 3114 | Vorinostat | HDAC inhibitor | €45.00 | |
| 3722 | Valemetostat | Inhibitor of Histone Lysine Methyltransferase EZH1/2 | Inquire | |
| 3288 | Vadadustat | Oral HIF-PH inhibitor and HIF stabilizer | €80.00 | |
| 2369 | UPF 1069 | PARP-2 inhibitor with >26 fold selectivity over PARP1 | €75.00 | |
| 3592 | UNC7145 | Negative control of UNC6934 as a chemical probe targeting NSD2-PWWP1 | €90.00 | |
| 3591 | UNC6934 | Potent and selective chemical probe targeting NSD2-PWWP1 | €120.00 | |
| 2163 | UNC669 | Antagonist of KMe reader protein L3MBTL1 and 3 | €70.00 | |
| 1994 | UNC1215 | Antagonist of L3MBTL3 methyllysine reader domain | €85.00 | |
| 1840 | UNC0646 | Inhibitor of G9a/GLP Histone Lysine Methyltransferase | €99.00 | |
| 1889 | UNC0638 | Inhibitor of G9a (EHMT2)/GLP (EHMT1) | €85.00 | |
| 1841 | UNC0631 | Inhibitor of G9a/GLP Histone Lysine Methyltransferase | €99.00 | |
| 2418 | UNC0379 | Substrate competitive inhibitor of the H4K20 HMTase SETD8 | €125.00 | |
| 1789 | UNC0224 | Inhibitor of G9a HMTase | €85.00 | |
| 2518 | UF 010 | Class I selective HDAC inhibitor that inhibits cancer cell proliferation | €60.00 | |
| 2893 | Tucidinostat | Orally bioavailable HDAC inhibitor (1, 2, 3, 10 Selective) | €95.00 | |
| 2004 | Tubastatin A hydrochloride | Potent and selective HDAC6 inhibitor | €95.00 | |
| 3691 | Tubacin | HDAC6 inhibitor | Inquire | |
| 2072 | Tofacitinib citrate | Potent Janus Kinase 3 (JAK3) inhibitor | €115.00 | |
| 2180 | TMP 195 | HDAC inhibitor (class IIA selective) | €110.00 | |
| 3402 | THZ531 | First-in-class, potent, selective, covalent CDK12/CDK13 inhibitor | €130.00 | |
| 2934 | TH 5487 | Potent and selective active-site OGG1 inhibitor | €125.00 | |
| 2996 | TH 34 | HDAC inhibitor (6, 8, 10 Selective) | €120.00 | |