EPZ005687

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

Product Specifications

CAS Number

[1396772-26-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/EPZ005687.html

Purity

99.46

Solubility

DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C3=CC=C(CN4CCOCC4)C=C3)=CC5=C2C=NN5C6CCCC6

Molecular Formula

C32H37N5O3

Molecular Weight

539.67

Precautions

H302, H315, H319, H335

References & Citations

[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.