EED226

Allosteric, Noncompetitive with SAM and peptide substrate of EED

Structure

Information

Protein target names: EED

Mechanism of action: Allosteric, Noncompetitive with SAM and peptide substrate

Recommended in-cell concentration:
100 nM - 1 uM

In Vitro Validations

Uniprot ID: O75530
Target Class: Epigenetic
Target SubClass: Polycomb family
Potency: Kd
Potency Value: 82 nM
Potency Assay: Isothermal titration calorimetry (ITC)
PDB ID for probe-target interaction (3D structure): 5GSA
Structure-activity relationship: Not available
Target aliases:
Polycomb protein EED, EED, EED_HUMAN, WAIT-1, hEED ...

DOI Reference: 10.1038/nchembio.2304

Uniprot ID: O75530
Target Class: Epigenetic
Target SubClass: Polycomb family
Potency: IC50
Potency Value: 23.4 nM
Potency Assay: In in vitro enzyme assays
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Polycomb protein EED, EED, EED_HUMAN, WAIT-1, hEED ...

DOI Reference: 10.1038/nchembio.2304

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating

SERP Comments:

The fact that this compound is non-competitive with respect to SAM and peptide substrate is supported by an X-ray structure and enzymatic competition assays. The furane ring with electron-donating group is supposed to be unstable, but the structure was confirmed to be stable under even an acidic condition reported in the supplementary note. I think the chemical probe could prove to be very interesting and useful.

(last updated: 13 Jun 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This allosteric inhibitor of PRC2 competes with the H3K27me3 peptide for binding to EED. So far, it seems to be a very clean inhibitor. The only data on this compound has been published by a single group, so validation by other groups will increase enthusiasm for its use as an orthogonal inhibitor to SAM-competitive EZH2 inhibitors now in clinical trials.

(last updated: 14 Jun 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 16 Jun 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 29 Aug 2017 )