EPZ005687

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Chemical Information

Product name：EPZ005687	Purity：98% min
CAS NO：1396772-26-1	Solubility：DMSO : 9.4 mg/mL (17.42 mM)
Molecular Formula：C₃₂H₃₇N₅O₃	Package：Package according to customer requirements
Molecular Weight：539.668	Storage：Store at -20℃

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Remarks

EPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM). EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against the closely related enzyme EZH1. The compound reduces H3K27 methylation in various lymphoma cells; this translates into apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells, with minimal effects on the proliferation of wild-type cells.

Histone Methyltransferase Inhibitors Related Products:

GSK343; Tazemetostat; UNC1999; MM-102; SGC0946; SGC2085; OICR-9429; HLCL-61 HCL; GSK591; SGC707; GSK503; EPZ015666; PFI-2 HCl; UNC0642; UNC0638; GSK-126; EPZ004777; GSK3326595; LLY-507; BRD4770; Pinometostat

References

[1]. Knutson SK, et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012;8(11):890-6.

[2]. Tang SH, et al. Effects of H3K27 methylation inhibitor EPZ005687 on apoptosis, proliferation and cell cycle of U937 cells and normal CD34 positive cells. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2014 Dec;22(6):1561-6.