Epigenetics

Axon Ligands™ for Epigenetic Research

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™ for Epigenetic research   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)

Histone Acetyltransferase (HAT)

DNA Methyltransferase (DNMT)

 


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
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 €95.00
2277 FLI 06 Notch signaling inhibitor that acts early in the secretory pathway €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 €110.00
1645 HDAC6 inhibitor ISOX HDAC6 Inhibitor €105.00
2096 Hesperadin Reversible and ATP-competitive inhibitor of Aurora B €95.00
1948 HIF Phd Inhibitor 4 Inhibitor of Hypoxia Inducible Factor PHD €105.00
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

Items 61 to 75 of 167 total

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