GSK 126
Tocris Bioscience, part of Bio-Techne | Catalog # 6790
Very high affinity and selective EZH2 inhibitor
Key Product Details
Description
Very high affinity and selective EZH2 inhibitor
Product Description
GSK 126 is a very high affinity and selective EZH2 inhibitor (Ki = 0.5 - 3 nM). Exhibits >150-fold selectivity for EZH2 over EZH1 and >1000-fold selectivity over 20 other human methyltransferases. Inhibits proliferation of B-cell lymphoma cell lines in vitro. Also inhibits H3K27Me3 and tumor growth in mice bearing BCL xenografts. Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection. Promotes the transition of ESCs to feeder-free extended pluripotent stem (EPS) cells in combination with LCDM cocktail.Product Specifications
Molecular Weight
526.67
Formula
C31H38N6O2
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide
CAS Number
1346574-57-9
PubChem ID
68210102
InChI Key
FKSFKBQGSFSOSM-QFIPXVFZSA-N
SMILES
CC[C@@H](N1C=C(C2=C(C(NCC3=C(C=C(NC3=O)C)C)=O)C=C(C4=CN=C(N5CCNCC5)C=C4)C=C12)C)C
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 | 2.63 | 5 with gentle warming |
Preparing Stock Solutions
for GSK 126
The following data is based on the product molecular weight 526.67
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 |
|---|---|---|---|
| 0.05 mM | 37.97 mL | 189.87 mL | 379.74 mL |
| 0.25 mM | 7.59 mL | 37.97 mL | 75.95 mL |
| 0.5 mM | 3.80 mL | 18.99 mL | 37.97 mL |
| 2.5 mM | 0.76 mL | 3.80 mL | 7.59 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Barili Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection. Nat.Commun. 2020 PMID: 32001678
- Zheng Derivation of feeder-free human extended pluripotent stem cells. Stem Cell Rep 2021 PMID: 34214484
- McCabe EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature 2012 PMID: 23051747
Product Specific Notices for GSK 126
For research use only
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