GSK 126

Name: GSK 126
Brand: Tocris Bioscience
SKU: 6790

Tocris Bioscience, part of Bio-Techne | Catalog # 6790

Citations (7)

COA / SDS

Very high affinity and selective EZH2 inhibitor

Key Product Details

Description:	Very high affinity and selective EZH2 inhibitor
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
Purity:	≥98% (HPLC)
Molecular Weight:	526.67

View Full Technical Details for GSK 126

Technical Data
Citations

Biological Activity for GSK 126

GSK 126 is a very high affinity and selective EZH2 inhibitor (K_i = 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.

Technical Data for GSK 126

M. Wt	526.67
Formula	C₃₁H₃₈N₆O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
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.

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

Solubility for GSK 126

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 will 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

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References for GSK 126

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