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
|
Histone Demethylase (LSD/Jumonji C) |
Histone Deacetylase (HDAC) |
|
SET domain lysine Methyltransferase (G9a/EZH2) |
Histone Deacetylase (SIRT) |
|
Arginine Methyltransferase (PRMT) |
|
|
DNA Methyltransferase (DNMT) |
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Recognition of modified Histone
|
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 | |
|---|---|---|---|---|
| 3061 | RBPJ inhibitor RIN1 | First-in-class, potent and selective RBPJ inhibitor | €120.00 | |
| 2299 | Remodelin | Potent NAT 10 inhibitor that mediates nuclear shape rescue in laminopathic cells via microtubule reorganization | €90.00 | |
| 1691 | RG 108 | DNA methyltransferase inhibitor | €80.00 | |
| 2195 | RGFP 966 | HDAC3 specific inhibitor | €85.00 | |
| 3113 | Rucaparib camsylate | PARP1 inhibitor | €90.00 | |
| 1598 | Ruxolitinib | JAK1 and JAK2 inhibitor | €65.00 | |
| 2245 | RVX 208 | BET bromodomain inhibitor specific for second bromodomains (BD2s) | €65.00 | |
| 2704 | Salermide | Potent inhibitor of SIRT1 and SIRT2 | €95.00 | |
| 2495 | Santacruzamate A | Picomolar level HDAC2 inhibitor with little inhibition of HDAC4 and HDAC6 | €85.00 | |
| 1777 | SB 939 | HDAC inhibitor (1, 2, 4 Selective) | €95.00 | |
| 2531 | SCR7 pyrazine | DNA ligase IV mediated inhibitor of NHEJ | €65.00 | |
| 1956 | Selisistat | Potent and selective SIRT1 inhibitor | €90.00 | |
| 2625 | SGC2085 | Potent and selective CARM1 inhibitor (aka PRMT4) | €120.00 | |
| 2945 | SGC707 | First-in-class, potent, selective and cell-active allosteric inhibitor of PRMT3 | €90.00 | |
| 2347 | SGI 1027 dihydrochloride | Inhibitor of DNMT activity in colon cancer cell lines | €110.00 | |
| 1633 | SGI 1776 free base | Pim kinase inhibitor | €95.00 | |
| 2453 | SirReal 2 | SIRT2 inhibitor with >1000 fold selectivity over SIRT1 and SIRT3 | €95.00 | |
| 2968 | SIRT7 inhibitor 97491 | Inhibitor of SIRT7 | €135.00 | |
| 2764 | SIS3 | Potent and selective inhibitor of Smad3 and TGF-βR1 signaling | €135.00 | |
| 1923 | SMI 4a | ATP-competitive and selective inhibitor of Pim kinases | €75.00 | |
| 2906 | SNS 314 mesylate | Potent and selective Aurora inhibitor (non-specific) | €90.00 | |
| 2209 | Sodium butyrate | Noncompetitive inhibitor of multiple histone deacetylases (HDACs) | €50.00 | |
| 2539 | Solcitinib | Selective JAK1 inhibitor for treatment of degenerative and inflammatory diseases | €90.00 | |
| 2864 | SP 2509 | Potent, reversible, and specific LSD1 inhibitor | €80.00 | |
| 1875 | SRT 1720 tetrahydrochloride | Activator of the sirtuin subtype SIRT1 | €95.00 | |
| 5008 | Stem Cell RG-BIX inhibitor Set | Set of RG 108 and BIX 01294 HCl, inhibitors of DNMT and HMTase, respectively | €60.00 | |
| 3587 | STM2457 | First-in-class, highly potent and selective catalytic METTL3 inhibitor | €170.00 | |
| 2263 | Tacrolimus | Potent Calcineurin (Ca2+ dependent protein phosphatase 2B) inhibitor | €100.00 | |
| 2502 | Talazoparib | Potent, selective, and orally available PARP1/2 inhibitor | €90.00 | |
| 2008 | Tenovin 1 | Activates p53 through inhibition of SIRT 1 and 2 | €70.00 | |