GSK343

Catalog No.S7164

GSK343 Chemical Structure

Molecular Weight(MW): 541.69

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.

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3 Customer Reviews

  • Representative confocal microscopy images of oocytes with DZNep or GSK343 treatment. The oocytes presented with a typical barrel-shaped spindle and well-aligned chromosomes on the metaphase plate not only in DZNep or GSK343 treated group but also in the control group. Spindle was recognized by α-tubulin (green) and DNA was recognized by PI (Propidium iodide, red). Scale bar = 4 μm.

    Nucleic Acids Res, 2016, 44(16):7659-72.. GSK343 purchased from Selleck.

    Ex vivo growth of the SCLC PDX LX92 is significantly inhibited by the EZH2 inhibitors EPZ-5687, GSK343 and UNC1999 as measured by resazurin conversion (two-way analysis of variance, adjusted for multiple comparisons by the method of Dunnet).

    Oncogene, 2015, 10.1038/onc.2015.38. GSK343 purchased from Selleck.

  • Western blot analysis for LIMK2b in H446DDP, H69AR cells inhibited EZH2 with EI1 or GSK343 or transfected with siRNA targeting EZH2 (si-NC, si-EZH2 1* and si-EZH2 2*).

    Mol Cancer, 2017, 16(1):5.. GSK343 purchased from Selleck.

Purity & Quality Control

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.
Features A chemical probe for the SGC epigenetics initiative. Potential use in a variety of solid tumors.
Targets
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  NETtXZdHfW6ldHnvckBCe3OjeR?= NGLTcVYxNjJ3LUKuNEDPxE1? NF\zc|k6PiCq NEXZT|lz\WS3Y3XzJJRwfGGuIHPlcIx2dGG{IITybY1mfGi7bHH0[YQhUDONMkegbY4h[SC2aX3lMUBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MXqyOlA1OTJ6Nx?=
MDA-MB-231 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrTNocxNTJyIN88US=> NXvXdJpDPzJiaB?= M3zQeJNpd3e|IHP5eI91d3irY3n0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVWzWY5iOjV{MEO2NlY>
MDA-MB-231 M4XiXGZ2dmO2aX;uJGF{e2G7 MUWxNEDPxE1? NX[zZ5hFPzJiaB?= NF3oSVFz\WS3Y3XzJJRp\SCuZY\lcEBw\iCKM1uyO{1u\TN? NV7LSYJyOjV{MEO2NlY>
MDA-MB-231 MYfGeY5kfGmxbjDBd5NigQ>? MWexNEDPxE1? MlXLO|IhcA>? NY\KVoN3cW6mdXPld{BNSzNvSVmgZYNkfW23bHH0bY9v M{LjUlI2OjB|NkK2
MDA-MB-231 NVXhcI9HTnWwY4Tpc44hSXO|YYm= M{jTfVExKM7:TR?= MmSzNlQhcA>? MXLpcoR2[2W|IHH1eI9xcGGpeR?= NEjud|kzPTJyM{[yOi=>
HepG2 NYjOVFBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrCR5AxNTJyIN88US=> NHrhV4o4OiCq Mnjod4hwf3NiY4n0c5RwgGmlaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MX6yOVIxOzZ{Nh?=
A549 NUTIR|JwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjqNJF{OC1{MDFOwG0> NGDtbJE4OiCq M1HmNpNpd3e|IHP5eI91d3irY3n0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVnJWZd[OjV{MEO2NlY>
HepG2 MoTaSpVv[3Srb36gRZN{[Xl? NGDlSWIyOCEQvF2= M{nm[FI1KGh? MkPkbY5lfWOnczDheZRweGijZ4m= NF\MfVkzPTJyM{[yOi=>
A549 NV;lPZFLTnWwY4Tpc44hSXO|YYm= MX2xNEDPxE1? NI\DSW8zPCCq NFO5RYhqdmS3Y3XzJIF2fG:yaHHnfS=> MYmyOVIxOzZ{Nh?=
OVCAR10 MlfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;jXlEh|ryP NVLWeXQ5OC1zMjDk NEXER|ZFVVOR MlzVbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M17QNVI{PzV7NUi5
UPN289 MlXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYSxJO69VQ>? MnXFNE0yOiCm MYfEUXNQ NHLOTFZqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 Mn7XNlM4PTl3OEm=
SKOV3  NF\iXmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSxJO69VQ>? NYmx[pFEOC1zMjDk NEftNoFFVVOR MoLkbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NEmybmIzOzd3OUW4PS=>
SKOV3  MnrBRZBweHSxc3nzJGF{e2G7 MmfCNUDPxE1? NHG1RlU1KGR? NFjNNJdFVVOR MlLJbY5lfWOnczDhdI9xfG:|aYOgZ5VtfHW{ZXSgbY4hO0RiY3;u[Il1cW:wcx?= MXeyN|c2QTV6OR?=

... Click to View More Cell Line Experimental Data

Protocol

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 DMF 10 mg/mL warmed (18.46 mM)
Ethanol 4 mg/mL (7.38 mM)
DMSO 1 mg/mL warmed (1.84 mM)

* 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
Formula

C31H39N7O2

CAS No. 1346704-33-3
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID