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
1338 CP 690550 JAK3 inhibitor €65.00
2594 CPI 0610 Selective and metabolically stable inhibitor of BET bromodomains Inquire
2622 CPI 4203 Selective inhibitor of KDM5 demethylases (H3K4 specific) €85.00
2573 CPI 455 Selective inhibitor of KDM5 demethylases (H3K4 specific) €95.00
2765 CPTH2 HAT inhibitor (Gcn5p specific) €125.00
2305 CX 6258 hydrochloride Pim kinase inhibitor €99.00
1681 CYT 387 JAK1 and JAK2 inhibitor €90.00
1590 Decitabine DNA methyltransferase inhibitor €85.00
1977 DMOG Cell-permeable HIF-PHD inhibitor with pro-angiogenic and -osteogenic properties €65.00
1268 DR 2313 PARP inhibitor €90.00
2701 EED226 Potent, selective and orally bioavailable PRC2 inhibitor €105.00
2568 EML 425 Potent reversible dual inhibitor of CBP and p300 (HAT/KAT3) €95.00
2737 EN460 Inhibitor of endoplasmic reticulum oxidation 1 (ERO1) €95.00
2831 EPZ 015666 Potent, selective and orally available inhibitor of PRMT5 €125.00
2227 EPZ 6438 Inhibitor of Histone Lysine Methyltransferase EZH2 €105.00

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