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EPZ005687

Catalog No. T1905 CAS 1396772-26-1

EPZ005687 is a potent and selective inhibitor of EZH2.

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EPZ005687, CAS 1396772-26-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 53.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 138.00
50 mg	In stock	$ 207.00
100 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 61.00

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Purity: 99.64%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	EPZ005687 is a potent and selective inhibitor of EZH2.
Targets&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.
Kinase Assay	Biochemical 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.
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)

Molecular Weight	539.67
Formula	C32H37N5O3
CAS No.	1396772-26-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.4 mg/mL (10 mM)

References and Literature

1. Knutson SK, et al. Nat Chem Biol, 2012, 8(11), 890-896.

Citations

1. Shishido K, Purvis I J, Velpula K K, et al.Targeting B7‑H3 through EZH2 inhibition in MYC‑positive Group 3 medulloblastoma.Oncology Reports.2023, 49(6): 1-13.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Histone Modification Compound Library Stem Cell Differentiation Compound Library Reprogramming Compound Library NO PAINS Compound Library Preclinical Compound Library Anti-Cancer Compound Library Methylation Compound Library

Related Products

Related compounds with same targets

XY1 Piribedil MS049 2HCl (1502816-23-0(free base)) UNC7096 Tanshindiol C EZH2-IN-15 GSK467 PRMT6-IN-3

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

EPZ005687 1396772-26-1 Chromatin/Epigenetic Histone Methyltransferase Inhibitor EPZ-005687 EPZ 005687 inhibit inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.