GSK343

SAM competitive inhibitor of EZH2

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 ratings)

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Information

Protein target names: EZH2

Mechanism of action: SAM competitive inhibitor

Recommended in-cell concentration:

100 nM - 3 uM

Primary References:

DOI - 10.1021/ml3003346

Probe Availability:

In Vitro Validations

Uniprot ID: Q15910

Target Class: Epigenetic

Target SubClass: Protein methyltransferase

Potency: Ki

Potency Value: 1.2 nM

Potency Assay: Ki app for SAM binding

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Histone-lysine N-methyltransferase EZH2, KMT6, EZH ...

DOI Reference: 10.1021/ml3003346

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 17 May 2016 )

SERP Ratings

In Cell Rating

Comments:

GSK343 is an excellent potent and selective EZH2 probe suitable for cell culture. Use in animals is limited due to it being PgP substrate.

(last updated: 18 May 2016 )

SERP Ratings

In Cell Rating

Comments:

The IC₅₀ is ~300 nM for reduction of H3K37me3 in HCC1806 cells. Use GSK343 in parallel with UNC1999 as an orthogonal probe.

(last updated: 30 May 2016 )