GSK 343

Name: GSK 343
Brand: Tocris Bioscience
SKU: 6128

Tocris Bioscience, part of Bio-Techne | Catalog # 6128

Citations (6)

COA / SDS

Potent and selective SAM-competitive EZH2 inhibitor

Key Product Details

Description:	Potent and selective SAM-competitive EZH2 inhibitor
Chemical Name:	N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	541.69

View Full Technical Details for GSK 343

Technical Data
Citations

Biological Activity for GSK 343

GSK 343 is a potent and selective SAM-competitive EZH2 inhibitor (IC₅₀ = 4 nM), that exhibits >60 fold selectivity for EZH2 over EZH1 and a range of other methyltransferases. GSK 343 decreases H3K27me3 levels in breast cancer cells and inhibits proliferation of prostate cancer cell lines in vitro.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the GSK343 probe summary on the SGC website.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GSK 343 is reviewed on the chemical probes website.

Technical Data for GSK 343

M. Wt	541.69
Formula	C₃₁H₃₉N₇O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1346704-33-3
PubChem ID	71268957
InChi Key	ULNXAWLQFZMIHX-UHFFFAOYSA-N
Smiles	CCCC1=C(C(NC(C)=C1)=O)CNC(C2=C3C=NN(C3=CC(C4=CC=NC(N5CCN(CC5)C)=C4)=C2)C(C)C)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GSK 343

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	10.83	20 with gentle warming

Preparing Stock Solutions for GSK 343

The following data is based on the product molecular weight 541.69.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	9.23 mL	46.15 mL	92.30 mL
1 mM	1.85 mL	9.23 mL	18.46 mL
2 mM	0.92 mL	4.62 mL	9.23 mL
10 mM	0.18 mL	0.92 mL	1.85 mL

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References for GSK 343

References are publications that support the biological activity of the product.

Scheer A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 2019 PMID: 30604761
Verma Identification of potent, selective, cell-active inhibitors of the histone lysine methyltransferase EZH2. ACS Med.Chem.Lett. 2012 PMID: 24900432