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
1989 (+)-JQ1

Potent and selective BET bromodomain inhibitor

€60.00
3822 (+)-JQ1 carboxylic acid (+)-JQ1 derivative; PROTAC precursor €110.00
3873 (-)-JQ-1 Inactive enantiomer of (+)-JQ1 €120.00
4192 (S)-BI 2536 Dual PLK1/BRD4 bromodomain inhibitor €170.00
2537 1,5-Isoquinolinediol PARP1 inhibitor and neuroprotective agent €50.00
1496 3-Aminobenzamide Competitive small molecule inhibitor of PARP €40.00
2705 A-196 Potent and selective inhibitor of SUV4-20 €105.00
3696 ABBV-075 Highly potent and orally bioavailable BET bromodomain (BRD) inhibitor €110.00
3956 ABBV-744 First-in-class highly BDII (Bromodomain II)-selective BET bromodomain inhibitor Inquire
3039 ACY-241 Selective and orally available HDAC6 inhibitor €120.00
1529 AG 014699 PARP1 inhibitor €60.00
1378 AG 490 JAK2 inhibitor €65.00
2746 AG-120 IDH1 mutant enzyme inhibitor €125.00
2745 AG-221 IDH2 mutant enzyme inhibitor €95.00
2274 AGI 6780 Potent and selective inhibitor of the tumor-associated mutant IDH2 (R140Q) €90.00
2389 AICAR Potent AMPK activator and inducer of differentiation of NSCs €45.00
2269 AK 1 Potent inhibitor of SIRT with good selectivity for SIRT2 over SIRT1 and SIRT3 €90.00
2270 AK 7 Potent, brain-permeable and selective inhibitor of SIRT2 €90.00
3834 Alantolactone STAT3 inhibitor; NLRP3 inhibitor €90.00
N0002 Althiomycin Antibacterial Inquire
1783 AMG 900 Aurora inhibitor (non-specific) €110.00
2863 AMI-1 Inhibitor of PRMT €99.00
2468 ANA 12 Selective TrkB antagonist with anxiolytic and antidepressant activity in mice €90.00
1490 Anacardic acid A HAT inhibitor €60.00
2394 AR-42 HDAC inhibitor €125.00
3944 ARV-825 Potent and selective protein BRD4 degrader Inquire
2219 AT 9283 Multitargeted kinase inhibitor (Aurora A/B, JAK2/3, and BCR-Abl) €85.00
1597 Aurora A inhibitor I Aurora A inhibitor €125.00
1630 Aurora A inhibitor II Aurora A inhibitor €125.00
5052 Axon Ligands™ Epigenetic compound library Axon Ligands™ Epigenetic compound library Inquire

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