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
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  Recently added €125.00
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
2369 UPF 1069 PARP-2 inhibitor with >26 fold selectivity over PARP1 €75.00
2163 UNC 669 Antagonist of KMe reader protein L3MBTL1 and 3 €70.00
1994 UNC 1215 Antagonist of L3MBTL3 methyllysine reader domain €85.00
1840 UNC 0646 Inhibitor of G9a/GLP Histone Lysine Methyltransferase €99.00
1889 UNC 0638 Inhibitor of G9a (EHMT2)/GLP (EHMT1) €85.00
1841 UNC 0631 Inhibitor of G9a/GLP Histone Lysine Methyltransferase €99.00
2418 UNC 0379 Substrate competitive inhibitor of the H4K20 HMTase SETD8 €125.00

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