For research use only.

Catalog No.S7164

28 publications

GSK343 Chemical Structure

CAS No. 1346704-33-3

GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy.

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Selleck's GSK343 has been cited by 28 publications

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Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy.
Features A chemical probe for the SGC epigenetics initiative. Potential use in a variety of solid tumors.
EZH2 [1]
(Cell-free assay)
EZH1 [1]
(Cell-free assay)
4 nM 240 nM
In vitro

GSK343 inhibits trimethylation of H3K27 (H3K27me3) with IC50 of 174 nM in HCC1806 breast cancer cells. GSK343 potently inhibits cell proliferation in breast cancer cells and prostate cancer cells, and the prostate cancer cell line LNCaP is the most sensitive to GSK343, with IC50 of 2.9 μM. [1] GSK343 significantly suppresses the growth of EOC cells cultured in 3D matrigel extracellular matrix (ECM), which mimics the tumor microenvironment in vivo. In addition, GSK343 also induces apoptosis of EOC cells in 3D and significantly inhibits the invasion of EOC cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
2D10  MX3GeY5kfGmxbjDBd5NigQ>? MW[wMlI2NTJwMDFOwG0> M{H1Rlk3KGh? NGeyWXRz\WS3Y3XzJJRwfGGuIHPlcIx2dGG{IITybY1mfGi7bHH0[YQhUDONMkegbY4h[SC2aX3lMUBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M{L4V|I3ODRzMki3
MDA-MB-231 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTpNE0zOCEQvF2= NEDOU3E4OiCq NEjIWml{cG:5czDjfZRwfG:6aXPpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYiyOVIxOzZ{Nh?=
MDA-MB-231 NELFbopHfW6ldHnvckBCe3OjeR?= M4HyV|ExKM7:TR?= MXG3NkBp M{PVTpJm\HWlZYOgeIhmKGyndnXsJI9nKEh|S{K3MY1mOw>? MmTMNlUzODN4Mk[=
MDA-MB-231 MlLPSpVv[3Srb36gRZN{[Xl? MojjNVAh|ryP NU\CVZFEPzJiaB?= Mlm1bY5lfWOnczDMR|MuUUliYXPjeY12dGG2aX;u NVH3enJjOjV{MEO2NlY>
MDA-MB-231 M4ThcGZ2dmO2aX;uJGF{e2G7 NXPSPJdxOTBizszN M2PNRlI1KGh? MV7pcoR2[2W|IHH1eI9xcGGpeR?= MVKyOVIxOzZ{Nh?=
HepG2 MmOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3HNE0zOCEQvF2= NYHJfnNGPzJiaB?= M2rWWZNpd3e|IHP5eI91d3irY3n0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYiyOVIxOzZ{Nh?=
A549 NIWzboRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnG2NE0zOCEQvF2= M1ywVFczKGh? MXzzbI94eyCleYTveI95cWOrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= Mm[0NlUzODN4Mk[=
HepG2 MoWxSpVv[3Srb36gRZN{[Xl? MV:xNEDPxE1? NUHjSndHOjRiaB?= M1\ZWYlv\HWlZYOgZZV1d3CqYXf5 NU\FXmVnOjV{MEO2NlY>
A549 MY\GeY5kfGmxbjDBd5NigQ>? MlHrNVAh|ryP MkK5NlQhcA>? NFnMNpdqdmS3Y3XzJIF2fG:yaHHnfS=> NVP1VIpWOjV{MEO2NlY>
OVCAR10 NV3DcZR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV:xJO69VQ>? MmL4NE0yOiCm MWfEUXNQ M2XSZYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NIm2cJczOzd3OUW4PS=>
UPN289 NYnKeGRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXZU3YyKM7:TR?= M1jVOVAuOTJiZB?= MlqwSG1UVw>? MYHpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MlvMNlM4PTl3OEm=
SKOV3  NWr0flZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHf0XmMyKM7:TR?= MoDINE0yOiCm M{H4O2ROW09? MUTpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MV2yN|c2QTV6OR?=
SKOV3  MYfBdI9xfG:|aYOgRZN{[Xl? NX;XbXF6OSEQvF2= MVm0JIQ> NUDkcIlrTE2VTx?= NU[1TFJtcW6mdXPld{BieG:ydH;zbZMh[3WudIXy[YQhcW5iM1SgZ49v\Gm2aX;udy=> MVmyN|c2QTV6OR?=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot

PubMed: 29228694     

Expression of H3K27me3 in U87 and LN229 cells treated with 5 μM GSK343 over time was determined by western blot analysis. GADPH was used as a loading control.

EZH2 / EED / SUZ12 ; 

PubMed: 29228694     

U87 and LN229 cells were treated with 5 μM GSK343 or 0.1% DMSO for 48 h and the levels of EZH2, EED, SUZ12, and GAPDH were examined by western blot analysis. 

N-cadherin / Vimentin / Snail / Slug / MMP2 / MMP9 ; 

PubMed: 29228694     

Protein levels of N-cadherin, Vimentin, MMP2, MMP9, Snail, Slug, and GAPDH in U87 and LN229 cells treated with 5 μM GSK343 or 0.1% DMSO for 48 h were examined by western blot analysis.

N-cadherin / H3K27me3 / Vimentin ; 

PubMed: 29228694     

Immunofluorescence staining of N-cadherin (green), Vimentin (green), and H3K27me3 (red) in U87 and LN229 cells after treatment with 5 μM GSK343 or 0.1% DMSO for 48 h.

Growth inhibition assay
Cell viability; 

PubMed: 26973856     

HepG2 cells were treated with 0-20 μM GSK343 for 72 h. Cell viability was examined by MTT assay.



Kinase Assay:[1]
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In vitro biochemical assays against histone methyltransferases:

Activity against EZH2 is assessed using 5 member PRC2 complex (Flag-EZH2, EED, SUZ12, AEBP2, RbAp48). The assay protocol may be summarized as follows: 10 mM stocks of compounds are prepared from solid in 100% DMSO. An 11 point serial dilution master plate is prepared in 384 well format (1:3 dilution, columns 6 and 18 were equal volume DMSO controls) and dispensed to assay ready plates using acoustic dispensing technology to create a 100 nL stamp of compound and DMSO controls. The assay additions consisted of equal volume additions of 10 nM EZH2 and the substrate solution (5 µg/mL HeLa nucleosomes and 0.25 µM [3H]-SAM) dispensed into assay plates using a multi-drop combi dispense. Reaction plates are incubated for 1 hr and quenched with an equal volume addition of 0.5 mg/mL PS-PEI Imaging Beads (RPNQ0098) containing 0.1 mM unlabeled SAM. The plates are sealed, dark adapted for 30 minutes, and a 5 minute endpoint luminescence image is acquired using a Viewlux imager. Plate statistics such as Z’ and signal to background as well as dose response curves are analyzed using Activity BaseXE. The in vitro biochemical activity of EZH1 is assessed as part of a 5 member PRC2 complex using a 384 well SPA assay identical to EZH2. Buffer components, reagent dispensing, compound plate preparation, quench conditions and data analysis are identical for EZH1 and EZH2 with final assay concentrations of 20 nM EZH1, 5 μM/mL HeLa nucleosomes and 0.25 μM [3H]-SAM. Further data analysis, pIC50 pivots and visualizations are enabled by TIBCO Spotfire. Compounds are profiled at Reaction Biology Corp. (Malvern, PA) to assess inhibition in their panel of histone methyltransferase assays. Methyltransferase activity is assessed using HotSpot technology, a miniaturized radioisotope-based filter binding assay. Inhibitors are dissolved in dimethyl sulfoxide (DMSO) and tested at concentrations up to 100 uM with a final DMSO concentration of 2%. Buffer containing the methyltrasferase at the listed concentration and its preferred substrate as shown in the accompanying table is preincubated with compound for 10 min. Reactions are initiated by the addition of 1 uM S-adenosyl-L-[methyl-3H]methionine (SAM), allowed to incubate for 60 min at 30C followed by transfer to P81 filter-paper and PBS wash before detection.
Cell Research:[1]
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  • Cell lines: Breast cancer cell lines (HCC1806, Sk-Br-3, ZR-75-1), prostate cancer cell lines (DU145, PC3, LNCaP)
  • Concentrations: ~50 μM
  • Incubation Time: 6 days
  • Method: To account for varying doubling rates among cancer cell lines, the optimal cell seeding is determined empirically for all cell lines by examining their growth in a 384-well plate over 6 days with a wide range of seeding densities. Cells are then plated at the optimal seeding density and allowed to adhere overnight. Cells are treated in duplicate with a 20-point 2-fold dilution series of compound or 0.147% DMSO (vehicle control) and incubated for 6 days at 37C in 5% CO2. Cells are then lysed with 25 μl CellTiter-Glo per well and chemiluminescence is quantified with a TECAN Safire2 microplate reader. In addition, an untreated plate of cells is harvested at the time of compound addition (T0) to quantify the starting number of cells. CTG values after 6 days of treatment were expressed as a percent of the T0 value and plotted against compound concentration. Data are fit with a 4-parameter equation to generate a concentration response curve and the concentration of compound required to inhibit 50% of growth (gIC50) is determined
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 1 mg/mL warmed (1.84 mM)
Water Insoluble
Ethanol '4 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 541.69


CAS No. 1346704-33-3
Storage powder
in solvent
Synonyms N/A
Smiles CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID