GSK 343
Tocris Bioscience, part of Bio-Techne | Catalog # 6128
Potent and selective SAM-competitive EZH2 inhibitor
Key Product Details
Description
Potent and selective SAM-competitive EZH2 inhibitor
Product Description
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.Product Specifications
Molecular Weight
541.69
Formula
C31H39N7O2
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for GSK 343
For research use only
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