Histone methyltransferase and demethylase inhibitors
Study the function of histone H3 methyltransferase and demethylase with these high quality and purified inhibitors.
Explore our best-selling histone H3 methyltransferase inhibitor
Study the function of histone H3 methyltransferase and demethylase with these high quality and purified inhibitors.
Histone H3 methyltransferase inhibitors
Histone methyltransferase (HMT) inhibitors can be grouped by their specificity for different types of methyltransferases. Both lysine and arginine HMTs use S-adenosylmethionine (SAM) as a co-factor and methyl group donor. Lysine-specific HMTs fall into two groups:
(1) Su(var)3-9, Enhancer of zeste, Trithorax (SET) domain-containing, which methylate lysines in the histone tails
(2) Non-SET domain containing, which methylate histone cores
Below, we list selected inhibitors that can be used to study the function of key SET domain-containing histone H3 HMTs:
3-deazaneplanocin A hydrochloride (DZNep)
Histone H3 demethylase inhibitors
Histone demethylase inhibitors can also be grouped by their specificity for different types of demethylases. Histone demethylases can be divided into 2 main groups:
(1) The flavin adenine dinucleotide (FAD)-dependent amine oxidases, such as the lysine-specific demethylase (LSD) family. These demethylate mono-and dimethylated substrates.
(2) The Fe(II) and α-ketoglutarate-dependent dioxygenases (2-oxoglutarate dioxygenases), which include the Jumonji C (JmjC) domain-containing family. These demethylate mono-, di- and trimethylated substrates.
Key histone H3 demethylase inhibitors and their specificities are described below.