SAM competitive inhibitor of EZH2



Protein target names: EZH2

Mechanism of action: SAM competitive inhibitor

Recommended in-cell concentration:
100 nM - 3 uM
Primary References:

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


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


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 )