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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Epigenetics>Histone Methyltransferase Inhibitors>EPZ005687
EPZ005687
  • EPZ005687

EPZ005687 NEW

Price $53 $77 $138
Package 5mg 10mg 25mg
Supply Ability: 10g
Update Time: 2026-06-02

Product Details

Product Name: EPZ005687 CAS No.: 1396772-26-1
Purity: 99.66% Supply Ability: 10g
Release date: 2026/06/02

Product Introduction

Bioactivity

NameEPZ005687
DescriptionEPZ005687, a potent and selective inhibitor of EZH2.
Cell ResearchPlating 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)
Kinase AssayBiochemical Enzyme Assays: Compound is incubated for 30 min with 40 μL per well of 5 nM PRC2 (final assay concentration in 50 μL is 4 nM ) in 1X assay buffer (20 mM Bicine [pH 7.6], 0.002% Tween-20, 0.005% Bovine Skin Gelatin and 0.5 mM DTT). 10 μL per well of substrate mix comprising assay buffer 3 H-SAM, unlabeled SAM, and peptide representing histone H3 residues 21-44 containing C-terminal biotin (appended to a C-terminal amide-capped lysine) are added to initiate the reaction (both substrates are present in the final reaction mixture at their respective Km values, an assay format referred to as ‘‘balanced conditions''. The final concentrations of substrates and methylation state of the substrate peptide are indicated for each enzyme Reactions are incubated for 90 min at room temperature and quenched with 10 μL per well of 600 μM unlabeled SAM, Then transferred to a 384-well flashplate and washed after 30 min.
In vitroEPZ005687 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.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information10% DMSO+90% Saline : 0.88 mg/mL (1.63 mM), Suspension.
DMSO : 8.82 mg/mL (16.34 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.85 mM), Sonication is recommended.
KeywordsInhibitor | inhibit | HistoneMethyltransferase | Histone Methyltransferase | EZH2 | EPZ-005687 | EPZ005687 | EPZ 005687
Inhibitors RelatedMAK-683 hydrochloride | SNDX-5613 | Tazemetostat | Piribedil | XY1 | UNC 0631 | (Iso)-Flavokawain A | EPZ015666 | iso-Azalansta | AMI-1 free acid | MS37452 | MRTX-1719
Related Compound LibrariesHighly Selective Inhibitor Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Chromatin Modification Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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TargetMol Chemicals Inc.

6YR United StatesUnited States
  • Since: 2011-01-07
  • Address: 36 Washington Street, Wellesley Hill, MA
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