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:
|Writer (mark added)||Inhibitor||Product code||Notes|
3-deazaneplanocin A hydrochloride (DZNep)
|Also inhibits trimethylation of H4K20 in vitro|
|EZH2 (H3K27me3)||UNC1999||ab146152||22-fold selectivity over EZH1|
|KMT1A/ SUV39 (H3K9me3)||Chaetocin||ab144534||Also inhibits other K9-specific HMTs|
|SET domain- containing HMTs||Sinefungin||ab144518||Non-selective inhibitor|
View our expanding range of HMT inhibitors here.
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.
|Eraser (mark removed)||Inhibitor||Product code||Notes|
|KDM6A/ UTX and KDM6B / JMJD3 (H3K27me3)|
Also inhibits other H3K27me3 demethylases and the H3K4me demethylases KDM5B/PLU1/JARID1B and KDM5C/Jarid1C/SMCX
|GSK-J2||ab144398||GSK-J1 isomer for use as a less-active control|
|GSK-J4||ab144395||Pro-drug of GSK-J1 for cellular use|
|GSK-J5||ab144397||Pro-drug of GSK-J2 for cellular use|
|KDM2/7 JMJC subfamily of histone demethylases||Daminozide||ab144621||Highly selective over other subfamily members (KDM3, KDM4, KDM5 and KDM6) and other 2-oxoglutarate oxygenases|
|JMJC-domain containing histone demethylases||IOX1||ab144394||Inhibits most 2-oxoglutarate oxygenases|
View all our inhibitors of histone modifying enzymes here.