GSK126

Catalog No.: A11757

EZH2 inhibitor

GSK126

GSK126 Chemical Structure

CAS NO. 1346574-57-9

GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes.

Availability: In stock

Package Price Qty
2 mg
$40.00
5 mg
$60.00
10 mg
$90.00
25 mg
$160.00
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Warning Products are for laboratory research use only. Not for human use. We do not sell to patients.
  • Lucy E. Dawson, .et al. Induction of Myogenic Differentiation Improves Chemosensitivity of Chemoresistant Cells in Soft-Tissue Sarcoma Cell Lines, Sarcoma, 2020, 2020: 8647981 PMID: 32300280
  • Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
  • Dupret B, .et al. The histone lysine methyltransferase Ezh2 is required for maintenance of the intestine integrity and for caudal fin regeneration in zebrafish, Biochim Biophys Acta Gene Regul Mech, 2017, Oct;1860(10):1079-1093 PMID: 28887218
  • Theresa Baker, .et al. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors, Oncotarget, 2015, Oct 20; 6(32): 32646-32655 PMID: 26360609

Biological Activity

GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes.
Targets
EZH2
9.9 nM
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 18.99 mL 94.94 mL 189.87 mL
0.5 mM 3.8 mL 18.99 mL 37.97 mL
1 mM 1.9 mL 9.49 mL 18.99 mL
5 mM 0.38 mL 1.9 mL 3.8 mL

*The above data is based on the productmolecular weight 526.67. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Catalog Num A11757
Actions Inhibitor
M. Wt 526.67
Formula C31H38N6O2
Solubility DMSO
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 1346574-57-9
Synonyms GSK 126, GSK-126
SMILES CC[[email protected]](C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C

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