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.

19 Item(s)

per page
Axon ID Name Description From price
2635 BAY-598 Selective inhibitor of SMYD2 €110.00
2735 BCI-121 Inhibitor of SMYD3 €90.00
1692 BIX 01294 trihydrochloride HMTase inhibitor (G9a and G9a-like protein) €80.00
2812 CM-272 First-in-class potent, selective and reversible inhibitor of G9a/DNMT €130.00
2227 EPZ 6438 Inhibitor of Histone Lysine Methyltransferase EZH2 €90.00
3960 EPZ-5676 Selective and S-adenosyl methionine (SAM) competitive inhibitor of DOT1L methyltransferase Inquire
4137 EPZ005687 hydrochloride EZH2 HMTase inhibitor Inquire
2140 GSK 126 Inhibitor of Histone Lysine Methyltransferase EZH2 €75.00
3469 MS1943 trifluoroacetate First-in-class EZH2 selective degrader; PROTAC €200.00
3695 PF-06821497 Inhibitor of Histone Lysine Methyltransferase EZH2 €160.00
5008 Stem Cell RG-BIX inhibitor Set Set of RG 108 and BIX 01294 HCl, inhibitors of DNMT and HMTase, respectively €60.00
1789 UNC0224 Inhibitor of G9a HMTase €85.00
2418 UNC0379 Substrate competitive inhibitor of the H4K20 HMTase SETD8 €125.00
1841 UNC0631 Inhibitor of G9a/GLP Histone Lysine Methyltransferase €99.00
1889 UNC0638 Inhibitor of G9a (EHMT2)/GLP (EHMT1) €85.00
1840 UNC0646 Inhibitor of G9a/GLP Histone Lysine Methyltransferase €99.00
3591 UNC6934 Potent and selective chemical probe targeting NSD2-PWWP1 €120.00
3592 UNC7145 Negative control of UNC6934 as a chemical probe targeting NSD2-PWWP1 €90.00
3722 Valemetostat Inhibitor of Histone Lysine Methyltransferase EZH1/2 Inquire

19 Item(s)

per page
Please wait...