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Chemical Structure| 1396772-26-1 Chemical Structure| 1396772-26-1

Structure of EPZ005687
CAS No.: 1396772-26-1

Chemical Structure| 1396772-26-1

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EPZ005687 is a potent inhibitor of PRC2 with IC50 value of 54±5nM (measured by PRC2 enzymatic activity), with selectivity >500-fold over other HMTs, ~50-fold over EZH1. EPZ005687 can specifically inhibit H3K27 methylation.

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Product Details of EPZ005687

CAS No. :1396772-26-1
Formula : C32H37N5O3
M.W : 539.67
SMILES Code : O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC4=C1C=NN4C5CCCC5)NCC6=C(C)C=C(C)NC6=O
MDL No. :MFCD25372029
InChI Key :ZOIBZSZLMJDVDQ-UHFFFAOYSA-N
Pubchem ID :60160561

Safety of EPZ005687

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of EPZ005687

epigenetics

Isoform Comparison

Biological Activity

Target
  • Histone Methyltransferase

    EZH2, Ki:24 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Synovial sarcoma cells 0.72 μM - 3.5 μM 72 h for wound healing; 14 days for cytotoxicity assessment inhibits proliferation and migration; reduces H3K27me3 levels PMC4850444
DLD1 cells 2.5 μM 24 h UNC1999 induced autophagy through transcriptional upregulation of LC3B gene. PMC5004071

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Balb/c mice Transverse aortic constriction (TAC)-induced pulmonary arterial hypertension model Intraperitoneal injection 10 mg/kg Once a week for 4 weeks EPZ005687 significantly inhibited the development of TAC-induced PAH through EZH2-SOD1-ROS dependent oxidative stress inhibition. PMC5960552

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.19mL

9.26mL

1.85mL

0.93mL

18.53mL

3.71mL

1.85mL

References

 

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