EZH2

Enhancer of zeste homolog 2 (EZH2) EC 2.1.1.43 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.

Products
Background
Literature

Inhibitors

Cat No Product Name / Activity
4703 3-Deazaneplanocin A hydrochloride
EZH2 histone methyltransferase inhibitor
6128 GSK 343
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)
4905 UNC 2400
Negative control of UNC 1999 (Cat. No. 4904)

Enhancer of zeste homolog 2 (EZH2) EC 2.1.1.43 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* or download your copy today!

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


    Epigenetics

    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

    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

    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

    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

    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

    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.