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
2223 Lomeguatrib Potent, orally active inhibitor of MGMT €135.00
2430 LW 479 HDAC inhibitor with cytotoxicity in a panel of breast cancer cell lines. €135.00
2480 LW6 Inhibitor of HIF-1α stability via MDH2 inhibition and/or binding with CHP1 €85.00
2554 LY 2784544 Potent, selective and ATP-competitive inhibitor of mutated janus kinase 2 (JAK2V617F) €95.00
1707 MC 1568 HDAC inhibitor (class IIA selective) €85.00
2759 ME0328 PARP3/ARTD3 inhibitor €95.00
1785 MG 149 HAT inhibitor (Tip60 and MOZ specific) €105.00
1961 MK 5108 Inhibitor of Aurora A kinase €110.00
2081 ML 324 dihydrochloride Inhibitor of JMJD2 histone demethylase €125.00
2733 ML329 Inhibitor of the MITF molecular pathway €105.00
2003 MLN 8237 Second generation selective Aurora A inhibitor €105.00
2505 Mocetinostat Class I selective HDAC inhibitor with broad spectrum antitumor activity €80.00
1803 MS 275 Inhibitor of HDAC (1 and 3 Selective) €80.00
2359 Nexturastat A HDAC6 inhibitor with good selectivity over HDAC1 and HDAC8 €95.00
2928 Niraparib Potent, selective, and orally available PARP1/2 inhibitor €105.00

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