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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EZH2
Available Sizes
Frequently Asked Questions
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