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EPZ005687

Chemical Structure : EPZ005687

CAS No.: 1396772-26-1

EPZ005687 (EPZ 005687)

Catalog No.: PC-21951Not For Human Use, Lab Use Only.

EPZ005687 is a potent, selective and SAM-competitive inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity over EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

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

Biological Activity

EPZ005687 is a potent, selective and SAM-competitive inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity over EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
EPZ005687 reduces H3K27 methylation in various lymphoma cells.
EPZ005687 suppresses cell proliferation and migration in sarcoma cell lines.

Physicochemical Properties

M.Wt 539.68
Formula C32H37N5O3
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

1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide

References

1. Knutson SK, et al. Nat Chem Biol. 2012 Nov;8(11):890-6.

2. Shen JK, et al. Sci Rep. 2016 Apr 29;6:25239.

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