High Quality, Purified Inhibitors to Study the Function of Histone H3 Methyltransferase and Demethylase

Introduction

Histone methyltransferase (HMT) inhibitors can be classified based on their specificity for various types of methyltransferases. Lysine and arginine HMTs both use S-adenosylmethionine (SAM) as a methyl group donor and co-factor. Lysine-specific HMTs can be classified into two groups:

  • Non-Su(var)3-9, Enhancer of zeste, Trithorax (SET) domain containing, which methylate histone cores
  • SET domain-containing, which methylate lysines in the histone tails

The following table lists selected inhibitors that can be used to investigate the function of key SET domain-containing histone H3 HMTs:

Writer (mark added)

Inhibitor

Product code

Notes

EZH2 (H3K27me3)

3-deazaneplanocin A

ab142215

lso inhibits trimethylation of H4K20 in vitro

3-deazaneplanocin A hydrochloride (DZNep)

ab145628

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

  1. The flavin adenine dinucleotide (FAD)-dependent amine oxidases, which include the lysine-specific demethylase (LSD) family. These inhibitors are used to demethylate mono-and dimethylated substrates.
  2. The Fe(II) and α-ketoglutarate-dependent dioxygenases (2-oxoglutarate dioxygenases), such as the Jumonji C (JmjC) domain-containing family. Mono-, di- and trimethylated substrates can be demethylated using these inhibitors.

The following table presents the key histone H3 demethylase inhibitors and their specificities:

Eraser (mark removed)

Inhibitor

Product code

Notes

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-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

Methylstat

ab144566

JIB-04

ab144818

About Abcam

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Last updated: Feb 5, 2018 at 5:09 AM

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