Covalent modifications of histone tails have fundamental roles in chromatin structure and function. One such modification, lysine methylation, has important functions in many biological processes that include heterochromatin formation, X-chromosome inactivation and transcriptional regulation. The DNA within our cells exists in the form of chromatin. The basic building block of chromatin is the nucleosome, a structure consisting of an octamer of four core histone proteins around which 147 base pairs of DNA is wrapped. Core histones are subject to a large number of covalent modifications (PTMs: Post Translational Modifications) including acetylation, methylation, phosphorylation and ubiquitination. Histone methylation occurs on arginine and lysine residues and is catalyzed by enzymes belonging to three distinct families of proteins: the protein arginine specific methyl transferase (PRMT1) family, the SET-domain-containing protein family, and the non-SET-domain proteins DOT1/DOT1L. Unlike acetylation, which generally correlates with transcriptional activation, histone lysine methylation can signal either activation or repression, depending on the sites of methylation. Similar to the discovery that bromodomains can recognize acetylated lysines, studies on histone methylation identified at least three protein motifs (the Chromo-, the Tudor-, and the WD40-repeat domain) that are capable of forming specific interactions with methylated lysine residues of histone[1],[2].

Histone methyltransferases listed: HMTasePRMT

[1] C. Martin, Y. Zhang. The diverse functions of histone lysine methylation. Nat. Rev. Mol. Cell Biol. 2005, 6, 838-849.
[2] E.L. Greer, Y. Shi . Histone methylation: a dynamic mark in health, disease and inheritance. Nat. Rev. Genetics 2012,  13, 343-357.

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2635 BAY-598 Selective inhibitor of SMYD2  Recently added €110.00
2735 BCI-121 Inhibitor of SMYD3  Recently added €90.00
1692 BIX 01294 trihydrochloride HMTase inhibitor (G9a and G9a-like protein) €80.00
2227 EPZ 6438 Inhibitor of Histone Lysine Methyltransferase EZH2 €105.00
2140 GSK 126 Inhibitor of Histone Lysine Methyltransferase EZH2 €75.00
5008 Stem Cell RG-BIX inhibitor Set Set of RG 108 and BIX 01294 HCl, inhibitors of DNMT and HMTase, respectively €70.00
1789 UNC 0224 Inhibitor of G9a HMTase €85.00
2418 UNC 0379 Substrate competitive inhibitor of the H4K20 HMTase SETD8 €125.00
1841 UNC 0631 Inhibitor of G9a/GLP Histone Lysine Methyltransferase €99.00
1889 UNC 0638 Inhibitor of G9a (EHMT2)/GLP (EHMT1) €85.00
1840 UNC 0646 Inhibitor of G9a/GLP Histone Lysine Methyltransferase €99.00

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