EPZ005687

SKU: orb1307167

Description

EPZ005687 is a small molecule research compound that selectively and potently inhibits the EZH2 methyltransferase. It is widely used in oncology research to study epigenetic mechanisms in both cellular and animal models of cancers, such as lymphomas.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1396772-26-1
• MW: 539.67
• Purity: 99.66%
• Formula: C₃₂H₃₇N₅O₃
• SMILES: Cc1cc(C)c(CNC(=O)c2cc(cc3n(ncc23)C2CCCC2)-c2ccc(CN3CCOCC3)cc2)c(=O)[nH]1
• Target: Histone Methyltransferase
• Solubility: DMSO:5.4 mg/mL (10.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.85 mM)

Bioactivity

• Target IC50:
  EZH2:24 nM(Ki)
• In Vitro:
  EPZ005687 directly inhibits the enzymatic activity of PRC2 without disrupting the protein-protein interactions among PRC2 subunits. It exhibits concentration-dependent inhibition of PRC2 enzymatic activity with an IC50 value of 54 nM. Additionally, EPZ005687 reduces H3K27 methylation in various lymphoma cell types and demonstrates potent cytotoxic effects in cells harboring Tyr641 or Ala677 mutations, while having minimal impact on the proliferation of wild-type cells. In lymphoma cell lines with the Tyr641 mutation, EPZ005687 causes derepression of known EZH2 target genes and affects genes specifically suppressed by the EZH2 Tyr641 mutant.
• Cell Research:
  Plating densities are determined for each cell line on the basis of linear log-phase growth. Cells are counted and split back to the original plating density in fresh medium with EPZ005687 on days 4 and 7.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Histone Methyltransferase, HistoneMethyltransferase, EPZ 005687, EPZ005687, EPZ-005687, EZH2, inhibit, Inhibitor

Compound Identifiers

PubChem CID

60160561