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
2852 BCI hydrochloride Allosteric inhibitor of dual-specificity phosphatases (DUSP) €75.00
2735 BCI-121 Inhibitor of SMYD3 €90.00
1692 BIX 01294 trihydrochloride HMTase inhibitor (G9a and G9a-like protein) €80.00
2306 Bizine Potent LSD1 inhibitor with selectivity over MAO-A/B, and LSD2 €120.00
2506 BMS 303141 Cell-permeable ATP-citrate lyase (ACL) inhibitor €90.00
2471 BRD 73954 Dual HDAC 6/8 inhibitor with excellent selectivity over the other HDACs €85.00
1781 C 646 HAT inhibitor (p300/CBP selective) €60.00
2210 C 7280948 Sulfone inhibitor of PRMT1 €85.00
2803 Cambinol Inhibitor of SIRT1 and SIRT2 €95.00
1836 CCT 137690 Aurora inhibitor (non-specific) €115.00
2699 CCT251236 HSF1 stress pathway inhibitor €145.00
2776 CD161 Potent, selective, and orally active BET bromodomain inhibitor €135.00
2014 CI 994 HDAC inhibitor that causes histone hyperacetylation in living cells €70.00
2184 CID 1067700 First inhibitor of Rab7 GTPase €125.00
2812 CM-272 First-in-class potent, selective and reversible inhibitor of G9a/DNMT €125.00

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