Epigenetics
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™ - Epigenetics Library.xls |
Modifiers of Histone
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Histone Demethylase (LSD/Jumonji C) |
Histone Deacetylase (HDAC) |
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SET domain lysine Methyltransferase (G9a/EZH2) |
Histone Deacetylase (SIRT) |
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Arginine Methyltransferase (PRMT) |
|
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DNA Methyltransferase (DNMT) |
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Recognition of modified Histone
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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 | |
|---|---|---|---|---|
| 2096 | Hesperadin | Reversible and ATP-competitive inhibitor of Aurora B | €95.00 | |
| 1948 | HIF Phd Inhibitor 4 | Inhibitor of Hypoxia Inducible Factor PHD | €105.00 | |
| 2034 | HIF-2 inhibitor 2 | Allosteric inhibitor of HIF-2 | €95.00 | |
| 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 | |
| 3860 | I-BET726 | Potent and selective, tetrahydroquinoline-based small molecule ligand binding to BET proteins | Recently added | Inquire |
| 3417 | IMT1B | First-in-class, potent and highly specific allosteric POLRMT inhibitor | €130.00 | |
| 1566 | Iniparib | PARP inhibitor | €60.00 | |
| 1921 | IOX2 | Inhibitor of Hypoxia Inducible Factor PHD | €95.00 | |
| 1843 | JAK2 inhibitor 13 | JAK2 inhibitor | €110.00 | |
| 2160 | JIB 04 | Jumonji histone demethylase inhibitor | €90.00 | |
| 2654 | JK184 | Hedgehog (Hh) signaling pathway antagonist with antiproliferative activity | €80.00 | |
| 3180 | JMJD6 inhibitor WL12 | First-in-class JMJD6 inhibitor | €95.00 | |
| 2529 | JNJ 26481585 dihydrochloride | Potent, orally available second-generation pan-HDAC inhibitor | €125.00 | |
| 3754 | JNJ-64619178 dihydrochloride | SAM-pocket binding (SAM Competitive) PRMT5 inhibitor | Inquire | |
| 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 | €90.00 | |
| 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 | |
| 3601 | Mandipropamid | Highly cell-permeable chemical inducer of proximity (CIP); Antifungal | €80.00 | |
| 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) | €90.00 | |
| 1961 | MK 5108 | Inhibitor of Aurora A kinase | €110.00 | |
| 3095 | MK-8617 | Potent, orally active pan-inhibitor of HIF-PHD | €90.00 | |