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
2614 HIF-2a Translation Inhibitor 76 HIF-2a translation inhibitor that works independent of mTOR €70.00
2710 HLCL65 hydrochloride Inhibitor of PRMT5 €105.00
1566 Iniparib PARP inhibitor €65.00
1921 IOX2 Inhibitor of Hypoxia Inducible Factor PHD €95.00
2537 Isoquinolinediol, 1,5- PARP1 inhibitor and neuroprotective agent €50.00
1843 JAK2 inhibitor 13 JAK2 inhibitor €105.00
2160 JIB 04 Jumonji histone demethylase inhibitor €90.00
2654 JK184 Hedgehog (Hh) signaling pathway antagonist with antiproliferative activity €80.00
2529 JNJ 26481585 dihydrochloride Potent, orally available second-generation pan-HDAC inhibitor €125.00
1989 JQ-1, (+)-

Potent and selective BET bromodomain inhibitor

€70.00
2809 KDM5 inhibitor compound 48 Selective and orally bioavailable KDM5 inhibitor €145.00
2001 KU 0058948 hydrochloride Potent and specific PARP1 inhibitor €135.00
2319 L 002 Inhibitor of p300 HAT (KAT3B) and p53 acetylation €80.00
2549 L67 Cytotoxic inhibitor of DNA ligase I and III €90.00
1548 LBH 589 HDAC1 Inhibitor €95.00

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