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Cat. No. Name Size Price Add Cart
KI2663GSK1265 mg$650
GSK12610 mg$1014
GSK12650 mg$1950
GSK126200 mg$4030

Chemical Characteristic

Product NameGSK126
SynonymsEZH2 inhibitor
CAS No.1346574-57-9
Molecular Weight 526.67
FormulaC31H38N6O2
Chemical Name1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide
Smilesn1(cc(c2c(cc(cc12)c1cnc(cc1)N1CCNCC1)C(=O)NCc1c(=O)[nH]c(cc1C)C)C)[C@H](CC)C
Chemical Structure

Biological activities

GSK126 is a potent and highly selective EZH2 inhibitor. GSK126 inhibits EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes.[1] The IC50 of GSK126 against EZH2-containing PRC2 is 9.9 nM.[2] In vitro, GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines. In vivo, GSK126 shows antilymphoma effect on human DLBCL cell line xenografts with complete growth inhibition at lower doses and tumor eradication at higher doses of drug.[1]

Protocols

In vitro, GSK126 is dissolved in DMSO.[1]

References

[1] Melnick A. Epigenetic therapy leaps ahead with specific targeting of EZH2. Cancer Cell. 2012, 22 (5): 569-570.
[2] Wang Z, Patel D J. Small molecule epigenetic inhibitors targeted to histone lysine methyltransferases and demethylases. 2013, 46 (4): 349-73.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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