All tags Histone H3 Histone methyltransferase and demethylase inhibitors

Histone methyltransferase and demethylase inhibitors

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:

Writer (mark added)Inhibitor
Product 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

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)InhibitorProduct codeNotes
KDM6A/ UTX and KDM6B / JMJD3  (H3K27me3)

GSK-J1

ab144396

Also inhibits other H3K27me3 demethylases and the H3K4me demethylases KDM5B/PLU1/JARID1B and KDM5C/Jarid1C/SMCX

GSK-J2ab144398GSK-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

View all our inhibitors of histone modifying enzymes here.

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. 
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