GSK343

GSK343 : SAM competitive inhibitor of EZH2

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

EZH2

SAM competitive

100 nM - 3 uM

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

Off-Target Selectivity Assesments

Potency assay (off target): EZH2 IC50 = 0.004 uM; SET7 IC50 = 63 uM; PRMT3 IC50 = 74 uM; All others IC50 > 100 uM (DNMT1, DNMT3A, DNMT3B, DOT1L, KMT2A, KMT2D, KMT2C, KMT2B, PRMT1, PRMT4, PRMT5, SETMAR, KMT5B, KMT5C, EHMT2)

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SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 17 May 2016 )

SERP Ratings

In Cell Rating

SERP 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

SERP 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 )

Portal Comments

In a 2023 study, Hu et al. evaluated GSK343 in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations equal or exceeding 1 uM. (DOI: 10.1016/j.chembiol.2023.09.003)

(last updated: 7 Nov 2023)