You are here:Home-Chemical Inhibitors & Agonists-Epigenetics-Histone Methyltransferase (HMTase)-GSK126
GSK126

Chemical Structure : GSK126

CAS No.: 1346574-57-9

GSK126 (GSK2816126A, GSK-126)

Catalog No.: PC-21939Not For Human Use, Lab Use Only.

GSK126 (GSK2816126A) is a potent, highly selective, and SAM-competitive inhibitor of EZH2 methyltransferase with IC50 of 9.9 nM.

Packing Price Stock Quantity
10 mg $98 In stock
25 mg $158 In stock
50 mg $248 In stock
100 mg $368 In stock
200 mg Get quote
1 g Get quote

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK126 (GSK2816126A) is a potent, highly selective, and SAM-competitive inhibitor of EZH2 methyltransferase with IC50 of 9.9 nM.
GSK126 potently inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (Kiapp = 0.5-3 nM).
GSK126 is more than 1,000-fold selective for EZH2 versus 20 other human methyltransferases, including both SET-domain-containing and non-SET-domain-containing methyltransferases, 150-fold selective over EZH1.
GSK126 decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice.

Physicochemical Properties

M.Wt 526.69
Formula C31H38N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-1-(sec-Butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide

References

1. McCabe MT, et al. Nature. 2012 Dec 6;492(7427):108-12.

2. De Martino M, et al. Cell Cycle. 2023 Dec-Dec;22(23-24):2552-2565.

Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

Contact Us sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

Get Quote

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • Additional Information: