SAH-EZH2

Pricing Availability   Qty
Cat.No. 6708 - SAH-EZH2 | N-Ac-Phe-Ser-Ser-Asn-Arg-[(S)-2-(4-pentenyl)alanine]-Lys-Ile-Leu-[(S)-2-(4-pentenyl)alanine]-Arg-Thr-Gln-Ile-Leu-Asn-Gln-Glu-Trp-Lys-Gln-Arg-Arg-Ile-Gln-Pro-Val (double bond covalent bridge: X-6-X-10) | CAS No. 1453222-26-8
Description: EZH2/EDD interaction inhibitor; suppresses PCR2 complex function
Datasheet
Citations
Reviews
Literature

Biological Activity

EZH2/EPP interaction inhibitor (Kd = 320 nM). Suppresses EZH2 expression and H3K27 trimethylation by PCR2 complex. Arrests proliferation and induces monocyte to macrophage differentiation of MLL-AF9 leukemia cell line.

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Technical Data

M. Wt 3432.05
Formula C155H256N48O40
Sequence FSSNRXKILXRTQILNQEWKQRRIQPV

(Modifications: Phe-1 = N-terminal Ac, X = (S)-2-(4-pentenyl)alanine, X-6 and X-10 stapled together with a double bond)

Storage Store at -20°C
CAS Number 1453222-26-8
Smiles [H][C@]([C@H](O)C)(C(N[C@H](C(N[C@@]([C@H](CC)C)(C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@]([C@H](CC)C)(C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(O)=O)C(C)C)=O)=O)CCC(N)=O)=O)[H])=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCC(N)=O)=O)CCCCN)=O)CC2=CNC3=CC=CC=C23)=O)CCC(O)=O)=O)CCC(N)=O)=O)CC(N)=O)=O)CC(C)C)=O)[H])=O)CCC(N)=O)=O)NC([C@@H](NC([C@@]4(CCC/C=C/CCC[C@](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(C)=O)CC5=CC=CC=C5)=O)CO)=O)CO)=O)CC(N)=O)=O)CCCNC(N)=N)=O)(C(N[C@H](C(N[C@@]([C@H](CC)C)(C(N[C@H](C(N4)=O)CC(C)C)=O)[H])=O)CCCCN)=O)C)C)=O)CCCNC(N)=N)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solubility Soluble to 1 mg/ml in water

References

References are publications that support the biological activity of the product.

Kim et al (2013) Targeted disruption of the EZH2-EED complex inhibits EZH2-dependent cancer. Nat.Chem.Biol. 9 643 PMID: 23974116

Kim et al (2015) SWI/SNF-mutant cancers depend on catalytic and non-catalytic activity of EZH2. Nat.Med. 21 1491 PMID: 26552009


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Keywords: SAH-EZH2, SAH-EZH2 supplier, EZH2, lysine, methyltransferase, EPP, interaction, inhibitors, inhibits, stapled, peptide, PCR2, complex, methylation, 6708, Tocris Bioscience

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Literature in this Area

Tocris offers the following scientific literature in this area 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.