Enhancer of zeste homolog 2 (EZH2) EC is a lysine methyltransferase and is the catalytic subunit of the PRC2 complex responsible for the methylation of histone H3. Overexpression of EZH2 has been linked multiple types of cancer.

Literature (6)
Gene Data

EZH2 Inhibitors

Cat. No. Product Name / Activity
4703 3-Deazaneplanocin A hydrochloride
EZH2 histone methyltransferase inhibitor
6790 GSK 126
Very high affinity and selective EZH2 inhibitor
6128 GSK 343
Potent and selective SAM-competitive EZH2 inhibitor
6153 JQEZ5
Potent and selective SAM-competitive EZH2 inhibitor
6169 PF 06726304 acetate
Highly potent and SAM-competitive EZH2 inhibitor
4904 UNC 1999
Potent and selective EZH2/EZH1 inhibitor
4930 UNC 2399
Biotinylated UNC 1999 (Cat.No. 4904)
5847 ZLD 1039
Potent and selective EZH2 inhibitor; orally bioavailable


Cat. No. Product Name / Activity
4905 UNC 2400
Negative control of UNC 1999 (Cat. No. 4904)

Enhancer of zeste homolog 2 (EZH2) EC is a lysine methyltransferase that catalyses the transfer of methyl groups from S-adenosylmethionine (SAM) to histone H3 at lysine 27. This facilitates the formation of heterochromatin and regulates gene expression.

EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2) complex which regulates cell fate. Methylation of H3 by the complex leads to silencing of target genes involved in cell cycle regulation, cell proliferation, cell differentiation and cancer progression. In human embryonic stem cells (hESCs), EZH2 plays roles in the maintenance of pluripotency, self-renewal, proliferation and differentiation.

Genetic, transcriptional and post-transcription dysregulation of EZH2 are frequently identified in cancers. Mutations and overexpression of EZH2 have been linked to breast, prostate and bladder cancer, as well as melanomas. Inhibition of EZH2 represents a potential therapeutic avenue as EZH2 inhibits tumor growth suppression genes.

External sources of pharmacological information for EZH2 :

Literature for EZH2

Tocris offers the following scientific literature for EZH2 to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Stem Cells Scientific Review

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Epigenetics Research Bulletin

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
Cancer Metabolism Poster

Cancer Metabolism Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Stem Cells Poster

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.

Enhancer of zeste 2

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
EZH2 Human EZH2 NM_004456 Q15910
Mouse Ezh2 NM_007971 Q61188
Rat Ezh2 NM_001134979 NP_001128451