GSK 126

Key Product Details

Product Description

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.

Product Specifications for GSK 126

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

Solubility

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.

Select a batch to recalculate based on the batch molecular weight:

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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

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 13 publications citing the usage of this 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 Documents for GSK 126