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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.

Last edited Thu 20 Oct 2022

​​​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)InhibitorProduct codeNotes
EZH2 (H3K27me3)3-deazaneplanocin A
3-deazaneplanocin A hydrochloride (DZNep)
ab142215
ab145628
Also inhibits trimethylation of H4K20 in vitro
EZH2 (H3K27me3)
UNC1999ab14615222-fold selectivity over EZH1
KMT1A/ SUV39 (H3K9me3)Chaetocinab144534Also inhibits other K9-specific HMTs
SET domain- containing HMTsSinefunginab144518Non-selective inhibitor

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)InhibitorProduct codeNotes
KDM6A/ UTX and KDM6B / JMJD3  (H3K27me3GSK-J1ab144396Also inhibits other H3K27me3 demethylases and the H3K4me demethylases KDM5B/PLU1/JARID1B and KDM5C/Jarid1C/SMCX
GSK-J2
ab144398GSK-J1 isomer for use as a less-active control
GSK-J4ab144395Pro-drug of GSK-J1 for cellular use
GSK-J5ab144397Pro-drug of GSK-J2 for cellular use
KDM2/7 JMJC subfamily of histone demethylasesDaminozideab144621Highly selective over other subfamily members (KDM3, KDM4, KDM5 and KDM6) and other 2-oxoglutarate oxygenases
JMJC-domain containing histone demethylasesIOX1ab144394Inhibits most 2-oxoglutarate oxygenases
Methylstatab144566 
JIB-04ab144818